2. Search Result
Search Result
Results for "

TRPV1 Antagonist

" in MedChemExpress (MCE) Product Catalog:

51

Inhibitors & Agonists

3

Peptides

2

Natural
Products

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 .
    TRPV1 antagonist 3
  • HY-109841
    Oleoyl serotonin

    		TRP Channel Neurological Disease
    Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1 .
    Oleoyl serotonin
  • 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.
    A-1165442
  • HY-111218
    TRPV1 antagonist 5

    		TRP Channel Neurological Disease
    TRPV1 antagonist 5 (compound 1) is a potent TRPV1 antagonist .
    TRPV1 antagonist 5
  • 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 .
    TRPV1 antagonist 7
  • 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 .
    TRPV1 antagonist 9
  • 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 .
    TRPV1 antagonist 6
  • 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 .
    (S)-ABT-102
  • 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 .
    (Rac)-AMG 628
  • 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 .
    TRPV1-Tat
  • HY-101736
    AMG9810
    4 Publications Verification

    		 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.
    AMG9810
  • 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 .
    AC4
  • 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 .
    BCTP
  • HY-100668
    JYL 1421

    SC 0030

    		 TRP Channel Neurological Disease
    JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.
    JYL 1421
  • HY-121122
    A778317

    		Others 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 .
    A778317
  • HY-108458
    SB 452533

    		TRP Channel Inflammation/Immunology
    SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8 .
    SB 452533
  • HY-15640
    Capsazepine
    Maximum Cited Publications
    34 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.
    Capsazepine
  • 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.
    AMG 517
  • 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 .
    AMG 7905
  • HY-12777
    Asivatrep

    PAC-14028

    		 TRP Channel Inflammation/Immunology
    Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.
    Asivatrep
  • HY-114017
    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 .
    Vanilloid receptor antagonist 1
  • 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 .
    A-425619
  • 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. 
    ABT-239
  • 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 .
    JNJ-17203212
  • 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.
    SB-705498
  • 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 .
    MK-2295
  • HY-12245
    SB-366791
    3 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 .
    SB-366791
  • 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 .
    AS1928370
  • 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 .
    AMG8163
  • 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 .
    JTS-653
  • 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) .
    AMG0347
  • 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 .
    Voacangine
  • 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 .
    DWP-05195
  • 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 .
    JNJ-39729209
  • 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 .
    L-R4W2
  • 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 .
    L-R4W2 TFA
  • 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).
    Stearoyl Serotonin
  • 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 (Ki=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 .
    Mavatrep
  • 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.
    CB2 receptor antagonist 1
  • HY-18662
    RQ-00203078
    3 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 .
    RQ-00203078
  • 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 .
    ABT-102
  • 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 .
    A-889425
  • 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 .
    BCTC
  • 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 .
    N-Arachidonoylserotonin
  • 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 .
    RN-1665
  • HY-12914
    V116517

    		TRP Channel Neurological Disease Inflammation/Immunology
    V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain .
    V116517
  • HY-131986
    LASSBio-1135

    		TRP Channel Neurological Disease Inflammation/Immunology
    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 .
    LASSBio-1135
  • HY-N6962
    α-Spinasterol

    		TRP Channel COX Bacterial Infection Neurological Disease Metabolic Disease
    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 .
    α-Spinasterol
  • HY-107436
    LE135
    1 Publications Verification

    		 RAR/RXR TRP Channel Neurological Disease Cancer
    LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5?μM and 20?μM, respectively .
    LE135
  • HY-169780
    (S)-AMG-628

    		TRP Channel Neurological Disease Inflammation/Immunology
    (S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca 2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models .
    (S)-AMG-628

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: