TRP Channel Antagonist

TRP Channel Antagonists (63):

Cat. No.	Product Name	Effect	Purity

HY-109087

Elismetrep	Antagonist	99.42%
Elismetrep (MT-8554) is a TRPM8 antagonist. Elismetrep reduces the frequency of vasomotor symptoms. Elismetrep can be used for study of pain.

HY-104059

AMG2850	Antagonist	99.89%
AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.

HY-100668

JYL 1421	Antagonist	99.54%
JYL 1421 is a TRPV1 receptor antagonist, with an IC₅₀ of 8 nM.

HY-110270

RN-9893	Antagonist	99.91%
RN-9893 is a potent and selective TRPV4 receptor antagonist with IC₅₀ values of 320, 420 and 660 nM for mouse, human and rat channels, respectively.

HY-145124

TRPM8 antagonist 3	Antagonist	99.51%
TRPM8 antagonist 3 is a novel TRPM8 blocker with an IC₅₀ value of 11 nM.

HY-108458

SB 452533	Antagonist	99.11%
SB 452533 is a potent and selective TRPV1 antagonist with the pK_b of 7.8.

HY-110199

TC-I 2014	Antagonist	≥99.0%
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC₅₀ values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.

HY-160603

PF-05214030	Antagonist	99.19%
PF-05214030 is a TRPV4 antagonist (IC₅₀: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist.

HY-12428

A-1165442	Antagonist	99.92%
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC₅₀ of 9 nM for human TRPV1.

HY-131986

LASSBio-1135	Antagonist	99.05%
LASSBio-1135 (Compound 3a) is an orally active TRPV1 antagonist. LASSBio-1135 is an anti-inflammatory and analgesic compound. LASSBio-1135 inhibits moderately the human PGHS-2 enzyme activity (IC₅₀ = 18.5 μM). LASSBio-1135 reverts the Capsaicin (HY-10448)-induced thermal hyperalgesia and reduces the carrageenan-induced rat paw edem.

HY-B0985A

Phenazopyridine	Antagonist	99.93%
Phenazopyridine is a competitive SARM1 inhibitor, with IC₅₀ 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine has a local anesthetic/analgesic effect. Phenazopyridine is used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine can promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases.

HY-103337

N-Arachidonoylserotonin	Antagonist	≥98.0%
N-Arachidonoylserotonin (Arachidonyl serotonin; AA-5-HT) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC₅₀ value of 1~12 µM. N-Arachidonoylserotonin acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels (IC₅₀=70~100 nM). N-Arachidonoylserotonin is analgesic in rodents .

HY-113654

AMG 7905	Antagonist
AMG 7905 is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 potentiates TRPV1 channels activation by protons and drives the reflectory inhibition of thermogenesis and tail-skin vasoconstriction, while potently blocking channel activation by capsaicin.

HY-142214

TRPA1-IN-1	Antagonist
TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.

HY-112202

GSK3395879	Antagonist
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC₅₀ of 1 nM for hTRPV4.

HY-111036

AMG0347	Antagonist
AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC₅₀ = 0.2 nm), protons (IC₅₀= 0.8 nm), or capsaicin (IC₅₀ = 0.7 nm).

HY-P10465

TRPV1-Tat	Antagonist
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain.

HY-121080

AMG8163	Antagonist
AMG8163 is an orally active antagonist for TRPV1. AMG8163 inhibits Capsaicin (HY-10448)-induced flinch in rats models, and exhibits anti-hyperalgesia effects in multiple pain models.

HY-W721480

HC-067047 hydrochloride	Antagonist
HC-067047 hydrochloride is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively.

HY-110270A

RN-9893 hydrochloride	Antagonist
RN-9893 Hydrochloride is an orally active antagonist of transient receptor potential vanilloid 4 (TRPV4), with IC₅₀ values of 0.42 and 0.66 μM, for humans and rats, respectively.

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