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TRPV1 Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Apoptosis (3) Bacterial (1) Cannabinoid Receptor (1) CGRP Receptor (2) COX (1) Cytochrome P450 (1) Endogenous Metabolite (1) FAAH (1) GLUT (1) Histamine Receptor (1) Insulin Receptor (2) Interleukin Related (1) Isotope-Labeled Compounds (1) Melatonin Receptor (2) Opioid Receptor (1) P2X Receptor (2) RAR/RXR (1) Reference Standards (2) Sodium Channel (2) TNF Receptor (1) TRP Channel (58) URAT1 (1)
By Research Areas:	Cancer (9) Cardiovascular Disease (1) Endocrinology (2) Infection (1) Inflammation/Immunology (15) Metabolic Disease (4) Neurological Disease (40)

By Targets:

5-HT Receptor (2)

Apoptosis (3)

Bacterial (1)

Cannabinoid Receptor (1)

CGRP Receptor (2)

COX (1)

Cytochrome P450 (1)

Endogenous Metabolite (1)

FAAH (1)

GLUT (1)

Histamine Receptor (1)

Insulin Receptor (2)

Interleukin Related (1)

Isotope-Labeled Compounds (1)

Melatonin Receptor (2)

Opioid Receptor (1)

P2X Receptor (2)

RAR/RXR (1)

Reference Standards (2)

Sodium Channel (2)

TNF Receptor (1)

TRP Channel (58)

URAT1 (1)

By Research Areas:

Cancer (9)

Cardiovascular Disease (1)

Endocrinology (2)

Infection (1)

Inflammation/Immunology (15)

Metabolic Disease (4)

Neurological Disease (40)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-144372

TRPV1 antagonist 3	TRP Channel	Neurological Disease
TRPV1 antagonist 3 (Compound 7q) is a potent *TRPV1* antagonist with an IC₅₀ of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .

HY-176063

TRPV1 antagonist 11	TRP Channel Opioid Receptor	Neurological Disease
TRPV1 antagonist 11 (compound 2ac) is a potent *TRPV1* antagonist with an IC₅₀ of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a K_i of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .

HY-111218

TRPV1 antagonist 5	TRP Channel	Neurological Disease
TRPV1 antagonist 5 (compound 1) is a potent *TRPV1* antagonist .

HY-161420

TRPV1 antagonist 7	TRP Channel	Neurological Disease
TRPV1 antagonist 7 (Compound 36) is a selective *TRPV1* antagonist that effectively blocks capsaicin activation (IC₅₀=2.31 nM). TRPV1 antagonist 7 can be used in analgesic research .

HY-172774

TRPV1 antagonist 10	TRP Channel URAT1 GLUT Cytochrome P450 Interleukin Related TNF Receptor	Neurological Disease Inflammation/Immunology Endocrinology
TRPV1 antagonist 10 is an orally active and potent *TRPV1* antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain .

HY-110091

TRPV1 antagonist 9	TRP Channel	Neurological Disease
TRPV1 antagonist 9 (compound 13c) is an orally active transient receptor potential vanilloid 1 (TRPV1) channel antagonist. TRPV1 antagonist 9 blocks Ca ²⁺ uptake by CHO cells expressing TRPV1 receptors with IC₅₀ values are 0.6 and 0.8 nM for Capsaicin (HY-10448) and acid-induced Ca ²⁺ uptake, respectively. TRPV1 antagonist 9 blocks Capsaicin (HY-10448)-induced flinch response and causes hyperthermia in rats .

HY-161273

TRPV1 antagonist 6	TRP Channel	Neurological Disease
TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC₅₀ of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration .

HY-10635A

(S)-ABT-102	TRP Channel	Inflammation/Immunology Cancer
(S)-ABT-102 is a *TRPV1* Antagonist, with an IC₅₀ of 123 nM. (S)-ABT-102 has analgesic activity .

HY-123374

(Rac)-AMG 628	TRP Channel	Neurological Disease
(Rac)-AMG 628 is the racemate of AMG 628, a potent *TRPV1* antagonist with an IC₅₀ of 3.7nM. AMG 628 can be used in chronic pain research .

HY-P10465

TRPV1-Tat	TRP Channel	Inflammation/Immunology
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-12428

A-1165442 2 Publications Verification	TRP Channel	Neurological Disease
A-1165442 is a potent, competitive and orally available *TRPV1* antagonist with an IC₅₀ of 9 nM for human TRPV1.

HY-109841

Oleoyl serotonin	TRP Channel	Neurological Disease
Oleoyl Serotonin (compound 1e) is a *TRPV1* antagonist with IC₅₀ value of 2.57 μM for human TRPV1 .

HY-101736

AMG9810 5+ Cited Publications	TRP Channel	Neurological Disease
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC₅₀ values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.

HY-110209

AC4	TRP Channel	Others
AC4 is a trans antagonist upon voltageactivation of *TRPV1* and as cis antagonist of *TRPV1* currents upon stimulation with Capsaicin (HY-10448). AC4 demonstrates that a photoswitchable antagonist and an agonist can be used in concert .

HY-117683

BCTP	TRP Channel	Neurological Disease
BCTP is a *TRPV1* antagonist. BCTP activated at low pH showed functional antagonist activity against human *TRPV1* in CHO cells (IC₅₀=18 nM). BCTP can be used in the study of chronic pain .

HY-100668

JYL 1421 SC 0030	TRP Channel	Neurological Disease
JYL 1421 is a TRPV1 receptor antagonist, with an IC₅₀ of 8 nM.

HY-121122

A778317	TRP Channel	Others
A778317 is a *TRPV1* antagonists. A778317 can block changes in intracellular calcium levels mediated by TRPV1 receptors, with a pIC₅₀ value of 8.31. A-778317 can also block the activation of natural rat TRPV1 receptors in dorsal root ganglion neurons by capsaicin and acid .

HY-108458

SB 452533	TRP Channel	Inflammation/Immunology
SB 452533 is a potent and selective *TRPV1* antagonist with the pK_b of 7.8 .

HY-15640

Capsazepine Maximum Cited Publications 43 Publications Verification	TRP Channel Apoptosis	Cancer
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC₅₀ of 562 nM.

HY-10634

AMG 517 5+ Cited Publications	TRP Channel	Neurological Disease
AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC₅₀ of 0.5 nM.

HY-113654

AMG 7905	TRP Channel	Others
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-12777

Asivatrep 1 Publications Verification PAC-14028	TRP Channel	Inflammation/Immunology
Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

HY-113654A

AMG 7905 TFA	TRP Channel	Cardiovascular Disease
AMG 7905 TFA is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 TFA 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-114017

Libvatrep SAF312; Vanilloid receptor Antagonist 1	TRP Channel	Inflammation/Immunology
Vanilloid receptor antagonist 1 is a potent vanilloid receptor *TRPV1* antagonist extracted from patent US8349852B2, compound B8 .

HY-110292

A-425619	TRP Channel	Inflammation/Immunology
A-425619, a potent and selective *TRPV1* receptor antagonist, is effective in alleviating acute and chronic inflammatory pain and postoperative pain .

HY-12195

ABT-239 2 Publications Verification	Histamine Receptor TRP Channel	Neurological Disease Endocrinology
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

HY-100129

JNJ-17203212 1 Publications Verification	TRP Channel	Neurological Disease
JNJ-17203212 is a selective, potent and competitive *TRPV1* antagonist. JNJ-17203212 is developed for researching pain management, such as migraine .

HY-W517163

MK-2295 NGD-8243	TRP Channel	Inflammation/Immunology
MK-2295 (NGD-8243) is a *TRPV1* antagonist. MK-2295 is an analgesic agent, and can be used for research of pain .

HY-10633

SB-705498 5+ Cited Publications	TRP Channel	Neurological Disease
SB-705498 is a potent, selective and orally bioavailable *transient receptor potential vanilloid 1 (TRPV1) receptor* antagonist with a pIC₅₀ of 7.1.

HY-12245

SB-366791 4 Publications Verification	TRP Channel	Inflammation/Immunology
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC₅₀=5.7 nM). SB-366791 can be used for the research of inflammation .

HY-15640R

Capsazepine (Standard)	TRP Channel Apoptosis	Cancer
Capsazepine (Standard) is the analytical standard of Capsazepine. This product is intended for research and analytical applications. Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.

HY-10634R

AMG 517 (Standard)	Reference Standards TRP Channel	Neurological Disease
AMG 517 (Standard) is the analytical standard of AMG 517. This product is intended for research and analytical applications. AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.

HY-124382

AS1928370	TRP Channel	Neurological Disease
AS1928370 is a novel and central nervous system (CNS) penetrant *TRPV1* antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research .

HY-121080

AMG8163	TRP Channel	Neurological Disease
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-19589

JTS-653	TRP Channel	Neurological Disease Inflammation/Immunology
JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents .

HY-111036

AMG0347	TRP Channel	Others
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-N7536

Voacangine	TRP Channel	Others
Voacangine is an antagonist for *TRPV1* and TRPM8 but as an agonist for TRPA1 (EC₅₀=8 μM). Voacangine competitively blockes capsaicin binding to *TRPV1* (IC₅₀=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC₅₀=9 μM) and it shows noncompetitive inhibition against icilin (IC₅₀=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .

HY-167868

DWP-05195	TRP Channel Apoptosis	Neurological Disease Cancer
DWP-05195 is a *TRPV1* antagonist that can inhibit the pain signal transduction. DWP-05195 induces ER stress-dependent apoptosis through the ROS-p38-CHOP pathway in human ovarian cancer cells .

HY-120476

JNJ-39729209	TRP Channel	Neurological Disease Inflammation/Immunology
JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC₅₀ of 7.9, 8.5, 7.9 and 7.7 for *TRPV1* from human, rat, canine and guinea pig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guinea pigs .

HY-P1175

L-R4W2	TRP Channel	Neurological Disease
L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 may act as a potent analgesic .

HY-P1175A

L-R4W2 TFA	TRP Channel	Neurological Disease
L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 TFA may act as a potent analgesic .

HY-121465

Stearoyl Serotonin	Endogenous Metabolite	Metabolic Disease
Stearoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of fatty acid amide hydrolase (FAAH) and the transient receptor potential vanilloid-type 1 (TRPV1) channel, reducing both acute and chronic peripheral pain. The effects of replacing the arachidonoyl portion with the saturated 18-carbon stearoyl moiety have not been studied. However, replacement of arachidonate with saturated 11- or 12-carbon fatty acids produces compounds that potently inhibit capsaicin-induced TRPV1 channel activation (IC₅₀=0.76 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC₅₀ > 50 μM).

HY-16935

Mavatrep JNJ-39439335	TRP Channel	Neurological Disease
Mavatrep (JNJ-39439335) is an orally active, selective and potent *TRPV1* antagonist with high affinity for hTRPV1 channels (K_i=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca ²⁺ influx with an IC₅₀ value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .

HY-147707

CB2 receptor antagonist 1	Cannabinoid Receptor	Others
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.

HY-133166

A-889425	TRP Channel	Neurological Disease
A-889425 is an oral active selective *TRPV1* receptor antagonist with the with an IC₅₀ of 335 nM (rat) and 34 nM (human). A-889425 has good penetration into the CNS and reduces mechanical allodynia and spinal neuron responses to mechanical stimulation of Complete Freund's adjuvant (HY-153808)-inflamed rat hind paws .

HY-18662

RQ-00203078 4 Publications Verification	TRP Channel	Neurological Disease Cancer
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC₅₀s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels .

HY-10635

ABT-102	TRP Channel	Inflammation/Immunology Cancer
ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain .

HY-19960

BCTC 4 Publications Verification	TRP Channel Insulin Receptor CGRP Receptor	Neurological Disease Metabolic Disease Cancer
BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects .

HY-103337

N-Arachidonoylserotonin Arachidonyl serotonin; AA-5-HT	FAAH TRP Channel	Neurological Disease
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-160900

RN-1665	TRP Channel	Others
RN-1665 is an orally active *TRPV4* antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P10465

TRPV1-Tat	TRP Channel	Inflammation/Immunology
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-P1175

L-R4W2	TRP Channel	Neurological Disease
L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 may act as a potent analgesic .

HY-P1175A

L-R4W2 TFA	TRP Channel	Neurological Disease
L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC₅₀ of 0.1 μM. L-R4W2 TFA may act as a potent analgesic .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N7536

Voacangine	Alkaloids Structural Classification other families Classification of Application Fields Source classification Other Diseases Plants Disease Research Fields Indole Alkaloids	TRP Channel
Voacangine is an antagonist for *TRPV1* and TRPM8 but as an agonist for TRPA1 (EC₅₀=8 μM). Voacangine competitively blockes capsaicin binding to *TRPV1* (IC₅₀=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC₅₀=9 μM) and it shows noncompetitive inhibition against icilin (IC₅₀=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .

HY-N6962

α-Spinasterol	Structural Classification Natural Products Plants Caryophyllaceae Melandrium firmum (S. et Z . ) Rohrb.	TRP Channel COX Bacterial
α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( *TRPV1), and it's also an inhibitor of COX-1* and COX-2, with IC₅₀ values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice .

Cat. No.	Product Name	Chemical Structure

HY-16935S

Mavatrep-d6
Mavatrep-d₆ (JNJ-39439335-d₆) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (K_i=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca ²⁺ influx with an IC₅₀ value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .

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