TRP ChannelTransient receptor potential channels

TRP Channel (Transient receptor potential channel) is a group of ion channels located mostly on the plasma membrane ofnumerous human and animal cell types There are about 28 TRP channels that share some structural similarity to each other Theseare grouped into two broad groups Group 1 includes TRPC (C for canonical) TRPV (V for vanilloid) TRPM (M for melastatin)TRPN and TRPA In group 2 there are TRPP (P for polycystic) and TRPML (ML for mucolipin) Many of these channels mediate avariety of sensations like the sensations of pain hotness warmth or coldness different kinds of tastes pressure and vision TRPchannels are relatively non-selectively permeable to cations including sodium calcium and magnesium TRP channels are initiallydiscovered in trp-mutant strain of the fruit fly Drosophila Later TRP channels are found in vertebrates where they are ubiquitouslyexpressed in many cell types and tissues TRP channels are important for human health as mutations in at least four TRP channelsunderlie disease

wwwMedChemExpresscom 1

TRP Channel Antagonists Inhibitors Agonists Activators amp Modulators

(-)-MentholCat No HY-75161

(-)-Menthol is a key component of peppermint oilthat binds and activates transient receptorpotential melastatin 8 ( ) aTRPM8Ca -permeable nonselective cation channel to2+

increase [Ca ] Antitumor activity2+i

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg 1 g

(E)-Cardamonin ((E)-Cardamomin (E)-Alpinetin chalcone) Cat No HY-N1378

(E)-Cardamonin ((E)-Cardamomin) is a novelantagonist of cation channel with an hTRPA1 IC50

of 454 nM

Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

(Z)-Capsaicin (Zucapsaicin Civamide cis-Capsaicin) Cat No HY-B1583

(Z)-Capsaicin is the cis isomer of capsaicin actsas an orally active agonist and is used inTRPV1the research of neuropathic pain

Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg

14-CineoleCat No HY-N7117

14-Cineole is a widely distributed naturaloxygenated monoterpene 14-Cineole present ineucalyptus oil activates both human andTRPM8human TRPA1

Purity gt950Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg

2-Aminoethyl diphenylborinate (2-APB) Cat No HY-W009724

2-Aminoethyl diphenylborinate (2-APB) is acell-permeable inhibitor of 2-AminoethylIP3Rdiphenylborinate also inhibits the store-operated

channel and activates some Ca (SOC)2+ TRPchannels (V1 V2 and V3)

Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg

8-GingerolCat No HY-N0447

8-Gingerol found in the rhizomes of ginger (Z) with oral bioavailability activatesofficinale

with an EC of 50 microM 8-GingerolTRPV1 50

inhibits COX-2 and inhibits the growth of H pyloriin vitro

Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg

A-1165442Cat No HY-12428

A-1165442 is a potent competitive and orallyavailable antagonist with an of 9 nMTRPV1 IC50

for human TRPV1

Purity 9970Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

A-967079Cat No HY-108463

A-967079 is a selective receptor antagonistTRPA1with s of 67 nM and 289 nM at human and ratIC50

TRPA1 receptors respectively and has goodpenetration into the CNS

Purity 9866Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

ABT-239Cat No HY-12195

ABT-239 is a novel highly efficaciousnon-imidazole class of antagonist and aH3Rtransient receptor potential vanilloid type 1( ) antagonist TRPV1

Purity 9906Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

Adenosine 5prime-diphosphoribose sodium (ADP ribose sodium) Cat No HY-100973A

Adenosine 5prime-diphosphoribose sodium (ADP ribosesodium) is a nicotinamide adenine nucleotide(NAD ) metabolite Adenosine 5prime-diphosphoribose+

sodium is the most potent and primaryintracellular Ca -permeable cation 2+ TRPM2

activatorchannel

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

2 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AM-0902Cat No HY-108329

AM-0902 is a potent selective transient receptorpotential A1 ( ) antagonist with s of 71TRPA1 IC50

and 131 nM for and respectivelyrTRPA1 hTRPA1

Purity 9967Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

AM12Cat No HY-128561

AM12 inhibits Lanthanide-evoked activityTRPC5with an of 028 μMIC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

AMG 333Cat No HY-112703

AMG 333 is a potent and highly selective TRPM8antagonist with an of 13 nMIC50

Purity 9976Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg

AMG 517Cat No HY-10634

AMG 517 is a potent and selective vanilloidreceptor-1 ( ) antagonist with an of 05TRPV1 IC50

nM

Purity 9997Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

AMG2850Cat No HY-104059

AMG2850 is a potent orally bioavailable andselective transient receptor potential melastatin 8

antagonist(TRPM8)

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

AMG9810Cat No HY-101736

AMG9810 is a selective and competitive vanilloidreceptor 1 ( ) antagonist with values ofTRPV1 IC50

245 and 856 nM for human and rat TRPV1repectively

Purity 9976Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Amiloride (MK-870) Cat No HY-B0285

Amiloride (MK-870) is an inhibitor of bothepithelial sodium channel ( ) andENaCurokinase-type plasminogen activator receptor( ) Amiloride is a blocker of uTPA polycystin-2(PC2 ) channelTRPP2

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Amiloride hydrochloride (MK-870 hydrochloride) Cat No HY-B0285A

Amiloride hydrochloride (MK-870 hydrochloride) isan inhibitor of both epithelial sodium channel( ) and urokinase-type plasminogen activatorENaCreceptor ( ) Amiloride hydrochloride is auTPAblocker of (PC2 ) channelpolycystin-2 TRPP2

Purity 9971Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg

Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) Cat No HY-B0285B

Amiloride hydrochloride dihydrate (MK-870hydrochloride dihydrate) is an inhibitor of bothepithelial sodium channel ( ) andENaCurokinase-type plasminogen activator receptor( ) Amiloride hydrochloride dihydrate is auTPAblocker of (PC2 ) channelpolycystin-2 TRPP2

Purity 9856Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Asivatrep (PAC-14028) Cat No HY-12777

Asivatrep (PAC-14028) is a potent and selectivetransient receptor potential vanilloid type I( ) antagonistTRPV1

Purity 9514Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg

wwwMedChemExpresscom 3

ASP7663Cat No HY-101907

ASP7663 is an orally active and selective TRPA1agonist ASP7663 exerts both anti-constipation andanti-abdominal pain actions

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

BCTCCat No HY-19960

BCTC is a potent and specific inhibitor oftransient receptor potential cation channelsubfamily M member 8 (TRPM8) in prostate cancer(PCa) DU145 cells

Purity 9723Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

Beta-EudesmolCat No HY-N6018

Beta-Eudesmol is a natural oxygenatedsesquiterpene activates with an hTRPA1 EC50

of 325 μM Beta-Eudesmol increases appetitethrough TRPA1

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg

BI-749327Cat No HY-111925

BI-749327 is a potent high selectivity and orallybioavailable antagonist with s of 13TRPC6 IC50

nM 19 nM and 15 nM for mouse human and guineapig TRPC6 respectively BI-749327 is 85-fold moreselective for mouse TRPC6 than TRPC3 and 42-foldversus TRPC7

Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Bisandrographolide CCat No HY-N2941

Bisandrographolide C is an unusual dimer ofent-labdane diterpenoid isolated and identifiedfrom Andrographis paniculata

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Caffeic acidCat No HY-N0172

Caffeic acid is an inhibitor of both ionTRPV1channel and ( )5-Lipoxygenase 5-LO

Purity 9880Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 5 g

Camphor ((plusmn)-Camphor) Cat No HY-N0808

Camphor ((plusmn)-Camphor) is a topical anti-infectiveand anti-pruritic and internally as a stimulantand carminative However Camphor is poisonouswhen ingested Antiviral antitussive andanticancer activities Camphor is a TRPV3agonist

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Capsaicin ((E)-Capsaicin) Cat No HY-10448

Capsaicin ((E)-Capsaicin) is a mixture ofCapsaicin and Dihydrocapsaicin Capsaici is a

agonist with an of 029 μM in HEK293TRPV1 EC50

cells

Purity 9901Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg

CapsazepineCat No HY-15640

Capsazepine is a synthetic analogue of the sensoryneurone excitotoxin and an antagonist of TRPV1

with an of 562 nMreceptor IC50

Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

Chembridge-5861528 (TCS 5861528) Cat No HY-15065

Chembridge-5861528 is a TRPA1 channel blocker thatantagonizes AITC- and 4-HNE-evoked calcium influx(IC50 values are 143 and 187μM respectively)

Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

4 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Cyclic ADP-ribose (cADPR) Cat No HY-N7395

Cyclic ADP-ribose (cADPR) is a potent secondmessenger for that iscalcium mobilizationsynthesized from NAD by a ADP-ribosyl cyclase+

Purity gt98Clinical Data No Development ReportedSize 500 μg

D-3263Cat No HY-16162

D-3263 is an agonist of transient receptorpotential melastatin member 8 ( ) withTRPM8potential antineoplastic activity

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg

D-3263 hydrochlorideCat No HY-16162A

D-3263 hydrochloride is an enteric-coated orallybioavailable (transient receptor potentialmelastatin member 8) agonistTRPM8

Purity 9801Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg

DihydrocapsaicinCat No HY-N0361

Dihydrocapsaicin is a natural capsaicin acts as aselective agonist and also increases p-AktTRPV1levels Dihydrocapsaicin enhances thehypothermia-induced neuroprotection

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg

Diphenyleneiodonium chloride (DPI) Cat No HY-100965

Diphenyleneiodonium chloride is a NADPH oxidase( ) inhibitor and also functions as a NOX TRPA1activator with an of 1 to 3 μMEC50

Diphenyleneiodonium chloride selectively inhibitsintracellular reactive oxygen species

Purity 9987Clinical Data Phase 4Size 10 mM times 1 mL 10 mg 50 mg 100 mg

DS88790512Cat No HY-112298

DS88790512 is a potent selective and orallybioavailable inhibitor with an of 11TRPC6 IC50

nM

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

EIPA (L593754 MH 12-43) Cat No HY-101840

EIPA (L593754) is a inhibitor withTRPP3 channelan of 105 μM EIPA also inhibitsIC50

( ) andNa H -exchanger+ + NHEmacropinocytosis

Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg

EIPA hydrochloride (L593754 hydrochloride MH 12-43 hydrochloride) Cat No HY-101840A

EIPA hydrochloride (L593754 hydrochloride) is a inhibitor with an of 105 μMTRPP3 channel IC50

EIPA hydrochloride also inhibits ( ) andNa H -exchanger+ + NHE

macropinocytosis

Purity 9939Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg

GFB-8438Cat No HY-133012

GFB-8438 is a potent and subtype selective TRPC5inhibitor with s of 018 and 029 μM ofIC50

hTRPC5 and hTRPC4 respectively GFB-8438 showsexcellent selectivity against TRPC6 other TRPfamily members NaV 15 as well as limitedactivity against the hERG channel

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

GSK1016790ACat No HY-19608

GSK1016790A is a potent transient receptorpotential vanilloid 4 ( ) activatorTRPV4

Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

wwwMedChemExpresscom 5

GSK1702934ACat No HY-111098

GSK1702934A is a selective agonistTRPC3GSK1702934A modulates cardiac contractility and farrhythmogenesis by activation of TRPC3

Purity gt990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

GSK205Cat No HY-120691A

GSK205 is a potent selective antagonistTRPV4with an of 419 μM for inhibitingIC50

-mediated Ca influxTRPV4 2+

Purity 9945Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

GSK2193874Cat No HY-100720

GSK2193874 is an orally active potent andselective antagonist with s of 2 nM andTRPV4 IC50

40 nM for and rTRPV4 hTRPV4

Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

GSK2798745Cat No HY-19765

GSK2798745 is a first-in-class highly potentselective orally active transient receptorpotential vanilloid 4 blocker(TRPV4) ion channelwith s of 18 and 16 nM for hTRPV4 andIC50

rTRPV4 respectively

Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg

GSK3395879Cat No HY-112202

GSK3395879 is a selective and orally bioavailabletransient receptor potential vanilloid-4 ( )TRPV4antagonist with an of 1 nM for hTRPV4IC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

HC-030031Cat No HY-15064

HC-030031 is a potent and selective TRPA1inhibitor which antagonizes AITC- andformalin-evoked calcium influx with s ofIC50

62plusmn02 and 53plusmn02 μM respectively

Purity 9591Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

HC-067047Cat No HY-100208

HC-067047 is a potent and selective TRPV4antagonist and reversibly inhibits currentsthrough the human rat and mouse orthologsTRPV4with values of 48 nM 133 nM and 17 nMIC50

respectively

Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

HC-070Cat No HY-112302

HC-070 is an antagonist of withTRPC4TRPC5s of 93 nM and 46 nM for hTRPC5 and hTRPC4 inIC50

cells respectively

Purity 9823Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

Hydroxy-α-sanshoolCat No HY-N6825

Hydroxy-α-sanshool is an alkylamide isolatedfrom acts as a covalent and pepper TRPA1 TRPV1non-covalent agonist with s of 69 and 11EC50

microM respectively

Purity gt950Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg

Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) Cat No HY-116330A

Hyperforin dicyclohexylammonium salt (HyperforinDCHA) is a transient receptor canonical 6 (TRPC6)channels activator Hyperforindicyclohexylammonium salt modulates Ca levels2+

by activating Ca -conducting non-selective2+

canonical TRPC6 channels

Purity 9817Clinical Data No Development ReportedSize 500 μg 1 mg

6 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

IA-Alkyne (Iodoacetamide-alkyne N-Hex-5-ynyl-2-iodo-acetamide) Cat No HY-136205

IA-Alkyne (Iodoacetamide-alkyneN-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel

agonist and has the potential for the(TRPC)study of respiratory infection IA-Alkyne can beused to develop an isotopically tagged forprobequantitative profilingcysteine-reactivity

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Icilin (AG-3-5) Cat No HY-11062

Icilin(AG 3-5) is a synthetic super-agonist ofTRPM8 ion channel

Purity gt960Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg

Imperatorin (Ammidin) Cat No HY-N0285

Imperatorin is an effective of NO synthesisinhibitor ( =92 μmol) which also is a IC50 BChEinhibitor ( =314 μmol) Imperatorin is a weakIC50

agonist of with of 126plusmn32 μMTRPV1 EC50

Purity 9581Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg

JNJ-17203212Cat No HY-100129

JNJ-17203212 is a novel and selective TRPV1antagonist with IC50 of 65 nM and 102 nM forhuman TRPV1 and rat TRPV1

Purity 9994Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

JT010Cat No HY-111132

JT010 is a potent agonist of with an TRPA1 EC50

of 065 nM

Purity 9921Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg

JYL 1421 (SC 0030) Cat No HY-100668

JYL 1421 is a antagonist with anTRPV1 receptor of 8 nMIC50

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Linopirdine (DuP 996) Cat No HY-W020468

Linopirdine (DuP 996) is an orally activeselective M-type K current (IM Kv7 KCNQ+

inhibitor with an of 24 μMChannels) IC50

Linopirdine is a agonist Linopirdine aTRPV1putative cognition enhancing drug increasesacetylcholine release in rat brain tissue

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Mavatrep (JNJ-39439335) Cat No HY-16935

Mavatrep is an orally bioavailable TRPV1antagonist (Ki=65 nM) exhibits minimal effect onthe enzymatic activity (IC50 gt 25 μM) of CYPisoforms 3A4 1A2 and 2D6

Purity 9985Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

MDR-652Cat No HY-136363

MDR-652 is a highly specific and efficacious ( )transient receptor potential vanilloid 1 TRPV1

ligand with agonist activity The s are 114 andKi

238 nM for hTRPV1 and rTRPV1 respectively Thes are 505 and 93 nM for hTRPV1 and rTRPV1EC50

respectively Potent topical analgesic activity

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Methyl syringateCat No HY-W002116

Methyl syringate a chemical marker of asphodelmonofloral honey is an efficient phenolicmediator for bacterial and fungal laccases Methylsyringate is a agonistTRPA1

Purity 9976Clinical Data No Development ReportedSize 100 mg

wwwMedChemExpresscom 7

Mifamurtide (MTP-PE L-MTP-PE CGP 19835) Cat No HY-13682

Mifamurtide (MTP-PE CGP19835) is a drug againstosteosarcoma Mifamurtide is an immunomodulatorwith antitumor effects that appear to be mediatedvia activation of monocytes and macrophages

Purity gt990Clinical Data LaunchedSize 1 mg 5 mg 10 mg

MK6-83Cat No HY-110238

MK6-83 is a new candidate agonist of TRPML1with an improved efficacy and potency MK6-83 hasthe potential for Mucolipidosis type IV study

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

ML204Cat No HY-12949

ML204 is a novel potent antagonist thatselectively modulates native TRPC4C5 ionchannels

Purity 9831Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

ML204 hydrochlorideCat No HY-12949A

ML204 hydrochloride is a novel potent selectiveTRPC4 channel inhibitor with IC50 of 096 uMexhibit 19-fold selectivity against TRPC6 channelsin similar fluorescent assays target ML204 IC50096 uM In vitro ML204 inhibited TRPC4β-mediatedintracellular Ca2+ rise

Purity 9964Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) Cat No HY-118628

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is abroad spectrum inhibitorPhospholipase A (PLA )2 2

and blockerTRP channel

Purity 9881Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg

Nonivamide (Pelargonic acid vanillylamide Nonanoic acid

vanillylamide Pseudocapsaicin) Cat No HY-17568

Nonivamide is a ltbltTRPV1 agonist whichexhibits 4d- value of 51 mgL in staticEC50

toxicity tests

Purity 9816Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg 5 g

OMDM-5Cat No HY-135881

OMDM-5 is a selective inhibitor of anandamide with a of 48 μMcellular uptake (ACU) Ki

OMDM-5 is also a potent vanilloid receptor type 1 agonist with an of 75 nM(VR1 TRPV1) EC50

and shows weakly active as cannabinoid receptortype 1 (CB1) ligand (K =49 μM)i

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

OMDM-6Cat No HY-135882

OMDM-6 is a hybrid agonist of vanilloid receptor ( =75 nM) and type 1 (VR1 TRPV1) EC50 cannabinoid

( =32 μM) OMDM-6receptor type 1 (CB1) Ki

inhibits withanandamide cellular uptake (ACU)a of 70 μMKi

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

OptovinCat No HY-12809

Optovin is a reversible photoactive TRPA1activator stimulates human TRPA1 channels invitro and enables repeated photoactivation ofmotor behaviors in wild-type zebrafish (EC50 = 2μM)

Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

PF-04745637Cat No HY-120689

PF-04745637 is a potent and selective TRPA1antagonist with an of 17 nM for human TRPA1IC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

8 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

PF-05105679Cat No HY-115506

PF-05105679 is an orally active and selective antagonist with an of 103 nMTRPM8 IC50

PF-05105679 has the potential for cold-relatedpain

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg

PF-4840154Cat No HY-18779

PF-4840154 is a potent selective agonist of therat and human channel with s of 97TrpA1 EC50

and 23 nM respectively

Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Pico145 (HC-608) Cat No HY-101507

Pico145 (HC-608) is a remarkable inhibitor of channels inhibits (minus)-englerinTRPC145

A-activated TRPC4TRPC5 channels with s ofIC50

0349 and 13 nM in cells and shows no effect onTRPC3 TRPC6 TRPV1 TRPV4 TRPA1 TRPM2 TRPM8

Purity 9942Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

Piromelatine (Neu-P11) Cat No HY-105285

Piromelatine (Neu-P11) is a melatonin receptor agonist MT MT1 2 serotonin

agonist and 5-HT1A 5-HT1D serotonin 5-HT2B

antagonist

Purity 9921Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Podocarpic acidCat No HY-N2318

Podocarpic acid is a natural product which hasthe best all-round positive effect and acts as anovel activatorTRPA1

Purity 9956Clinical Data No Development ReportedSize 10 mg 50 mg

ProbenecidCat No HY-B0545

Probenecid is a potent and selective agonist oftransient receptor potential vanilloid 2 ( )TRPV2channels Probenecid also inhibits pannexin 1channels

Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 500 mg 1 g 5 g

PulegoneCat No HY-N1500

Pulegone the major chemical constituent of (L) Savi essential oil whichCalamintha nepeta

is an aromatic herb with a mint-oregano flavor isone of avian repellents The molecular target forthe repellent action of Pulegone in avian speciesis nociceptive TRP ankyrin 1 (TRPA1)

Purity 9966Clinical Data No Development ReportedSize 5 mg

Pyr10Cat No HY-19408

Pyr10 is a pyrazole derivative and a selective inhibitor Pyr10 inhibitsTRP cation 3 (TRPC3)

Ca influx in carbachol-stimulated2+

-transfected HEK293 cells with an ofTRPC3 IC50

072 μM (IC of 1308 μM for store operated Ca502+

entry in BRL-2H3 cells)

Purity 9960Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg

Pyr3Cat No HY-108465

Pyr3 is a selective inhibitor of transientreceptor potential canonical channel 3 (TRPC3)with an of 700 nM for TRPC3-mediated CaIC50

2+

influx

Purity 9989Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg

Pyr6Cat No HY-12504

Pyr6 is a selective inhibitor of TRPC3 with IC50of 049 uM(Ca2+ influx inhibition in thapsigargindepleted native RBL-2H3 cells) IC50 value 049uM Target TRPC3 inhibitor Pyr6 is a selectiveSOCE inhibitor (Yonetoku et al 2008 Sweeney etal

Purity 9942Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg

wwwMedChemExpresscom 9

Resolvin D2 (RvD2) Cat No HY-121636

Resolvin D2 is a metabolite of docosahexaenoicacid (DHA) with anti-inflammatory anti-infectiveactivities Resolvin D2 is a potent regulator ofleukocytes and controls microbial sepsis

Purity gt98Clinical Data No Development ReportedSize 25 μg 50 μg

RN-1734Cat No HY-19975

RN-1734 is selective antagonist of the TRPV4 completely antagonizes 4αPDD-mediatedchannel

activation of TRPV4 with comparable lowmicromolar s for all three species (hTRPV4IC50

23 μM mTRPV4 59 μM rTRPV4 32 μM)

Purity 9901Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

RN-1747Cat No HY-19976

RN-1747 is a selective transient receptor potentialcation channel subfamily V member 4 (TRPV4)agonist with values are 077 μM 40 μMEC50

and 41 μM for hTRPV4 mTRPV4 and rTRPV4respectively RN-1747 also antagonizes TRPM8 withan IC of 4 μM50

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Rosiglitazone (BRL 49653) Cat No HY-17386

Rosiglitazone (BRL 49653) a Thiazolidinedioneinsulin sensitizer is a selective orally active

agonist with s of 30 nM 100 nM andPPARγ EC50

60 nM for PPARγ1 PPARγ2 and PPARγ respectivelyRosiglitazone binds to PPARγ with a ofKd

approximately 40 nM

Purity 9921Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 200 mg

Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Rosiglitazone maleate (BRL 49653C) is a potent andselective activator of with s of 30PPARγ EC50

nM 100 nM and 60 nM for andPPARγ1 PPARγ2 respectively and a of appr 40 nM forPPARγ Kd

Rosiglitazone maleate is also an modulatorPPARγof inhibits TRP melastatinhellipTRP channels

Purity 9975Clinical Data LaunchedSize 100 mg 500 mg

RQ-00203078Cat No HY-18662

RQ-00203078 is a highly selective potent andorally available TRPM8 antagonist (IC50 values are53 and 83 nM for rat and human channelsrespectively) exhibits gt350-fold selectivityfor TRPM8 over TRPV4 TRPV1 and TRPA1

Purity 9935Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

SAR7334Cat No HY-15699

SAR7334 is a potent and specific inhibitorTRPC6inhibiting TRPC6 currents with of 79 nMIC50

Purity 9991Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

SAR7334 hydrochlorideCat No HY-15699A

SAR7334 hydrochloride is a potent and specific inhibitor inhibiting TRPC6 currents withTRPC6

of 79 nMIC50

Purity 9561Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

SB-366791Cat No HY-12245

SB-366791 is a potent competitive and selectivevanilloid receptor (VR1TRPV1) antagonist withIC50 of 57plusmn12 nM target VR1TRPV1 IC 5057plusmn12 nM SB-366791 produced aconcentration-dependent inhibition of the responseto capsaicin with an apparent pKb ofhellip

Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

SB-705498Cat No HY-10633

SB-705498 is a potent selective and orallybioavailable transient receptor potential vanilloid

antagonist with a of1 (TRPV1) receptor pIC50

71

Purity 9961Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

10 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SKF-96365 hydrochlorideCat No HY-100001

SKF-96365 hydrochloride is a non-selective TRP blockerChannel

Purity 9944Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg

SN 2Cat No HY-16696

SN 2 is a novel and potent activator of TRPML3ion channel with of 18plusmn013 μMEC50

Purity 9999Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg

TC-I 2014Cat No HY-110199

TC-I 2014 (compound 5) is a potent and orallyactive Benzimidazole-containing transient receptor

antagonist withpotential melastatin 8 (TRPM8) values of 08 nM 30 nM and 44 nM forIC50

canine human and rat channels respectively

Purity gt990Clinical Data No Development ReportedSize 5 mg

TRPA1 Antagonist 1Cat No HY-111494

TRPA1 Antagonist 1 is a methylene phosphateprodrug which converts to its active parent druga antagonist with an of 8 nMTRPA1 IC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

TRPC6-IN-1Cat No HY-101547

TRPC6-IN-1 is a Transient Receptor PotentialCanonical 6 Channel inhibitor with an(TRPC6)

of 466 μMEC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

TRPC6-PAM-C20Cat No HY-136190

TRPC6-PAM-C20 is a selective positiveTRPC6allosteric modulator TRPC6-PAM-C20 selectivelyactivates TRPC6 over other TRP channels and alsoactivates TRPA1 TRPC6-PAM-C20 induces transientincrease in intracellular Ca in HEK cells2+

expressing TRPC6 ( =237 μM)EC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

TRPM8 antagonist 2Cat No HY-112430

TRPM8 antagonist 2 is a potent and selective antagonist with an of 02 nM usedTRPM8 IC50

in the research of neuropathic pain syndromes

Purity 9820Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

TRPM8 antagonist WS-3Cat No HY-W014325

TRPM8 antagonist WS-3 is an agonist of TRPM8with an of 37 μMEC50

Purity 9921Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg

TRPV antagonist 1Cat No HY-U00330

TRPV antagonist 1 is a transient receptorpotential vanilloid antagonist with an(TRPV)

of lt 250 nMIC50

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

TRPV4 agonist-1Cat No HY-114400

TRPV4 agonist-1 is a transient receptor potentialvanilloid 4 (TRPV4) agonist with an EC of 60 nM50

in the hTRPV4 Ca assay2+

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

wwwMedChemExpresscom 11

UmbelluloneCat No HY-135013

Umbellulone is an active constituent of the leavesof UmbelluloneUmbellularia californicastimulates the in a subset ofTRPA1 channelpeptidergic nociceptive neurons activating thetrigeminovascular system via this mechanism

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Vanilloid receptor antagonist 1Cat No HY-114017

Vanilloid receptor antagonist 1 is a potentvanilloid receptor antagonist extractedTRPV1from patent US8349852B2 compound B8

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

WS-12Cat No HY-108449

WS-12 is an agonist of with an ofTRPM8 EC50

39 nM

Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg

α-SpinasterolCat No HY-N6962

α-Spinasterol isolated from hasSpinacia oleraceaantibacterial activity α-Spinasterol is atransient receptor potential vanilloid 1 ( )TRPV1antagonist has anti-inflammatory antidepressantantioxidant and antinociceptive effects

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

12 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom