LY3526318 is an orally active, selective TRPA1 antagonist (IC50=5-6μM). LY3526318 blocks TRPA1 channels, inhibits pain signal transduction mediated by the channel, and exerts analgesic activity. LY3526318 is mainly used in the research of chronic pain-related fields, such as diabetic peripheral neuropathy, chronic low back pain, and pain caused by osteoarthritis.

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.

SA-13353 is a TRPV1 agonist with cardioprotective effect. SA-13353 can be used for the research of cardiovascular disease .

ABT-116 is an orally active antagonist of transient receptor potential vanilloid type 1 (TRPV1). ABT-116 has analgesic efficacy. ABT-116 can be used for the research of neurological disease.

SAR-115740 is a TRPV1 antagonist. SAR-115740 exhibits developmental toxicity in H9 cell experiments. SAR-115740 can be used for research on inflammatory conditions or neurological disorders.

SK2220691 is a potent TRPV4 inhibitor. SK2220691 inhibits pulmonary edema induced by GSK1016790. SK2220691 inhibits HCl-induced increases in key factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF).

ZA18 is a selective TRPM2 channel inhibitor, with an IC50 value of 6.2 μM. ZA18 can effectively suppress intracellular Ca2+ overload triggered by TRPM2 channel activation. ZA18 significantly reduce the mortality of SH-SY5Y cells induced by H2O2. ZA18 can be used for the study of ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

8-Br-cADPR (8-Bromo-Cyclic ADP-Ribose) sodium salt, a cyclic adenosine diphosphate (ADP)-ribose (cADPR) antagonist, is a TRPM2 ion channel antagonist. 8-Br-cADPR sodium salt reduces renal damage and the expression of caspase-3 and TRPM2.

PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC50  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.

HZS60 is a NMDAR/TRPM4 inhibitor with brain permeability that can improve cerebral ischemia. HZS60 has significant neuroprotective effects on primary neuronal ischemic damage caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 exhibits good pharmacokinetic characteristics and can inhibit cerebral ischemia-reperfusion injury. HZS60 can be used as a potential inhibitor of ischemic stroke.

ZQMT-10 is an orally active and potent antagonist of TRPA1, with the Kd of 1.04 μM. ZQMT-10 plays an important role in cancer research.

Davasaicin (KR 25018), Capsaicin derivative and a δ-opioid receptor agonist. AZ 12488024 is available for research into major depressive disorder.

CMP233 is a potent antagonist of TRPM4, with the IC50 of 0.15 μM. CMP233 plays an important role in neurodegenerative disorders research.

(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628. (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin- and acid-induced Ca2+-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-induced inflammatory pain models.

AMG9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM).

AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.

JNJ-28583113 (JNJ28583113) a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).JNJ-28583113 shows similar potency against species chimpanzee and rat TRPM2 with IC50 of 100 and 25 nM, respectively.JNJ-28583113 shows no significant (IC50>10 uM) reactivity towards PARP or PARG and a panel for multiple known kinases GPCRs and ion channels, nine other TRP channels with exception of TRPM5 (IC50<1 uM).Blocking TRPM2 via JNJ-28583113 caused phosphorylation of GSK3α and β subunits in cell assays.JNJ-28583113 also protected cells from oxidative stress induced cell death as well as morphological changes induced by non-cytotoxic concentrations of H2O2。JNJ-28583113 blunted cytokine release in response to pro-inflammatory stimuli in microglia.JNJ-28583113 was brain penetrant but not suitable for systemic dosing as it was rapidly metabolized in vivo, but the in-vitro pharmacology of JNJ-28583113 is the best in class.

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.

ZINC 17988990 is a potent, selective inhibitor of TRPV5 mediated currents, inhibits rbTRPV5/hTRPV5 with IC50 of 106/177 nM, showing marked selectivity for TRPV5 over TRPV6.ZINC 17988990 shows no activity on other TRP channels (TRPV1, TRPV3, TRPV4 and TRPM8) at 1-3 uM, and moderate inhibition on TRPV3 and TRPM8 at >10 uM.ZINC17988990 (10 uM) fully inhibited Ca2+ signals elicited by application of external Ca2+ in HEK293 cells transfected with TRPV5, but had no effect in cells expressing TRPV6.

AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.

VPC01091.4 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 0.665 uM.

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

Triphenylphosphine oxide (TPPO) is a selective and potent inhibitor of TRPM5 with IC50 of 12 and 30 uM for human and murine TRPM5 heterologously expressed in HEK293 cells.

SAR7334 (SAR-7334 ) is a highly potent and selective inhibitor of TRPC6 channel, reduces TRPC6-mediated Ca2+ influx with IC50 of 9.5 nM.

M085 (TRPC3/6/7 activator 4o) is a potent and selective TRPC3/6/7 activator with EC50 of 4.66 uM, also activates hTRPC6 with EC50 of 3.8 uM.

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.

KS0365 (KS 0365) is a potent and selective activator of transient receptor potential vanilloid 3 (TRPV3) channel with EC50 of 5.08 uM.

JNc-463 is a small-molecule that could increase the TRPV4-eNOS interaction, enhances vasodilation and exert antihypertensive effects in mice.

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.