|Description||ABT 102 is a selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with IC50 values to be 5-7 nM. No recent reports of development identified for phase-I development in Pain in USA.|
|Quality Standard||In-house standard|
|Current Developer||Originator Abbott Laboratories|
RQ-00203078 is a potent, selective and orally active TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). RQ-00203078 bloc...
AP18 is a selective Transient receptor potential A1(TRPA1) channel blocker which reversibly inhibits TRPA1 with IC50 values of 3.1 and 4.5 µM at human and mouse...
GSK1016790A is a novel and potent transient receptor potential vanilloid 4 (TRPV4) agonist. It has been used to demonstrate a role for TRPV4 in regulating urina...
PF-4840154 has been foundd to be superior than Mustard Oil as a TrpA1 agonists. IC50: 97 nM and 23 nM (EC50) for hTrpA1 and rTrpA1 respectively.
Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-ty...
ABT 102 is a selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with IC50 values to be 5-7 nM. No recent reports of development iden...
SAR7334, a TRPC6 inhibitor, could be valuable in studying sorts of diseases related to TRPC.
SN 2 is a novel and potent small molecule activator of TRPML3. Its EC50 value is 1.13 uM. It had a similar synergistic effect and reached up-to 10-fold enhancem...
The hydrochloride salt form of SAR7334, a TRPC6 inhibitor, could be valuable in studying sorts of diseases related to TRPC.
PF-05105679 is a selective TRPM8 Antagonist with clinical efficacy in cold-related pain. IC50 value is 103 nM. It shows >100-fold selectivity for TRPM8 over a p...
Capsazepine, a benzazepine derivative, has been found to be a sensory neurone excitotoxin that could be used against hyperalgesic responses. IC50: 562 nM (Rat T...
ML204 is a novel and potential TRPC4 Channel inhibitor. ML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited ...
SB-366791 is a potent, and selective cinnamide TRPV1 antagonist (pA2 = 7.71 at hVR1) with IC50 of 5.7±1.2 nM.
Pyr6, a pyrazole derivative, is a selective inhibitor of ransient receptor potential cation 3 (TRPC3) channels that inhibited Orai1- and TRPC3-mediated Ca(2+) e...
Capsaicin, the major pungent ingredient found in hot red chili peppers of the genus Capsicum, suppresses the growth of several malignant cell lines.
BCTC is a TRPA1 and TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.
MK-2295 is a potent TRPV1 antagonist. TRPV1 antagonists has the potential as analgesic and anti-inflammatory agents.
WS12 is a potent TRPM8 agonist. It acts as a cooling agent with EC50 value of 193 nM. It robustly activated TRPM8 in low micromolar concentrations, thus display...
AMG8562 is a novel vanilloid receptor TRPV1 modulator.
SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of volta...