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    TRP Channel

    TRP Channel (Transient receptor potential channel) is a group of ion channels located mostly on the plasma membrane of numerous human and animal cell types. There are about 28 TRP channels that share some structural similarity to each other. These are 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 a variety of sensations like the sensations of pain, hotness, warmth or coldness, different kinds of tastes, pressure, and vision. TRP channels are relatively non-selectively permeable to cations, including sodium, calcium and magnesium. TRP channels are initially discovered in trp-mutant strain of the fruit fly Drosophila. Later, TRP channels are found in vertebrates where they are ubiquitously expressed in many cell types and tissues. TRP channels are important for human health as mutations in at least four TRP channels underlie disease.

    Products

    Catalog No. Name Description
    GY07312 New GSK3395879 GSK3395879 is selective and orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) with IC50 of 1 nM.
    GY03284 Special SB-366791 SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nM target: VR1/TRPV1 IC 50: 5.7±1.2 nM [1] SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08.
    GY03845 Special HC-030031 HC-030031 is a potent and selective of TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
    GY01789 SKF-96365 HCl SKF-96365 hydrochloride, a potent TRP Channel blocker, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells.
    GY01847 GSK1016790A GSK101 (GSK1016790A) is a novel TRPV4 activator.
    GY01995 ML204 HCl ML204 is a novel, potent, selective TRPC4 channel inhibitor with IC50 of 0.96 uM. exhibit 19-fold selectivity against TRPC6 channels in similar fluorescent assays.
    GY02184 Ethylisopropylamiloride EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
    GY02312 RQ-00203078 RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
    GY03212 Icilin Icilin(AG 3-5) is a synthetic super-agonist of TRPM8 ion channel.
    GY03228 WS-3 WS-3 is an agonist of TRPM8 with an EC50 of 3.7 μM.
    GY03485 WS-12 WS-12 is an agonist of TRPM8 with an EC50 of 39 nM.
    GY03568 Mifamurtide (CGP-19835) Mifamurtide(CGP19835; MTP-PE) is a drug against osteosarcoma.
    GY03647 HC-067047 HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 ± 6 nM, 133 ± 25 nM, and 17 ± 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM).
    GY03705 JT010 JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.
    GY04001 Mavatrep Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
    GY04027 TCS5861528 Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively).
    GY04074 Optovin Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-type zebrafish (EC50 = 2 μM).
    GY05054 RN-1734 A potent, selective TRPV4 antagonist with IC50 of 2.3, 3.2 and 5.9 uM for hTRPV4, rTRPV4 and mTRPV4 channels, respectively.
    GY05090 SN-2 A small molecule activator of the TRPML3 ion channel with EC50 of 1.13 uM.
    GY05092 JNJ-17203212 A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.
    GY05130 AMG-9810 A potent, selective and competitive TRPV1 antagonist with IC50 of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
    GY05138 SB-705498 A potent, selective and orally bioavailable TRPV1 antagonist with pKi of 7.6 (inhibition of capsaicin-mediated activation of hTRPV1 receptor).
    GY05177 Nonivamide A capsaicin analog that acts as an agonist of TRPV1 channel.
    GY05251 Pico145 Pico145 is a highly potent, subtype-selective TRPC1/4/5 channels inhibitor with potency ranged from 9 to 1300 pM, depending on the TRPC1/4/5 subtype and activation mechanism.
    GY05290 AMG-333 AMG-333 (AMG333, AMG 333) is a novel potent, highly selective TRPM8 antagonist with IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively.
    GY05295 PF-05105679 PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).
    GY05305 GSK 2833503A GSK 2833503A (GSK2833503A, GSK503A) is a potent, and selective inhibitor of TRPC3/6 channels with IC50 of 4 nM/5 nM, respectively.
    GY05306 GSK 2332255B GSK 2332255B (GSK2332255B, GSK255B) is a potent, and selective inhibitor of TRPC3/6 channels with IC50 of 3 nM/21 nM, respectively.
    GY05312 GSK-2193874 GSK-2193874 (GSK2193874) is an orally active, potent, and selective blocker of TRPV4 channel with IC50 of 40 nM and 2 nM for hTRPV4 and rTRPV4, respectively.
    GY05314 PF-4840154 A potent, selective agonist of the rat (EC50=97 nM) and human (EC50=23 nM) TRPA1 channel.
    GY05379 Asivatrep Asivatrep (PAC-14028) is a potent, selective TRPV1 antagonist with IC50 of 55 nM against capsaicin-induced Ca2+ influx in rat DRG neurons, does not inhibit or activate other TRP channels such as hTRPV2, hTRPV3, hTRPM8 and hTRPA1.
    GY07074 MRS 1477 A small molecule positive allosteric modulator of both proton and vanilloid activation of TRPV1 (EC50=21.3 uM)
    GY06935 2-APB A membrane permeable IP3 receptor antagonist and broad TRP channels (TRPC5, TRPM2) blcoker.