Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels.
CIM0216, a potent and selective agonist of TRPM3, has the ability to open two distinct cation-permeable pores in TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts as a powerful tool for use in investigating the physiological roles of TRPM3, and can be used for neurogenic inflammation research[1].
Methyl syringate-d6 is the deuterium labeled Methyl syringate[1]. Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist[2][3][4].
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM[1].
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model[1][2][3][4][5].
HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons[1][2][3].
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model[1].
The compound inhibits TRPC proteins, and more specifically inhibits the TRPC6 protein.
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM)[1].
Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research[1].
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca2+ influx in macrophages, and inhibits macrophage phagocytosis[1].
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM[1].
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD+ by a ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels[1].
AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM; demonstrates high aqueous solubility (pH6.8, >100 uM), satisfactory stability in human liver microsomes, and reduced CYP3A4 inhibition; improves capsaicin-induced secondary hyperalgesia and mechanical allodynia in an L5/L6 spinal nerve ligation model in rats with respective ED50s of 0.17 and 0.26 mg/kg p.o.
TRPM8-IN-1 (example 14) is an inhibitor of transient receptor potential melastatin-8 (TRPM8) channels, IC50<5 μM[1].
AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.Target: TRPM8in vitro: BCTC is a potent and specific antagonist of TRPM8, exerts an anti-tumor effect on the androgen-independent PCa DU145 cells, and the mechanism of how the inhibition functions. BCTC exerts an anti-proliferative effect on DU145 cells and induces tumor suppression through G0/G1 cell cycle arrest, and inhibition of migration and invasion. BCTC demonstrates excellent anti-tumor activity in PCa DU145 cells, and therefore has the potential to become a targeted therapeutic strategy against PCa. [1]in vivo: BCTC is a potent, selective, and orally bioavailable antagonist of rat VR1. BCTC not only blocks the activation of rat VR1 by capsaicin but also by low pH at the native rat VR1 in a skin-nerve preparation. Thus, BCTC has provided us with an opportunity to test our hypothesis that the inhibition of low pH induced activation of VR1 confers in vivo efficacy in models of chronic pain. This report describes the effects of BCTC in models of inflammatory, neuropathic, and capsaicin-induced pain in the rat. The efficacy and side effect profile of BCTC in these models were compared with those of nonsteroidal anti-inflammatory drugs and antiepileptic drugs currently used for the clinical therapy of inflammatory and neuropathic pain, respectively.[2]
Vocacapsaicin (CA-008) hydrochloride, a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride can provide meaningful and long-lasting pain relief[1].
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1[1].
N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). N-oleoyl-glutamine is a transient receptor potential (TRP) antagonist[1].
GSK1016790A is a potent transient receptor potential vanilloid 4 (TRPV4) activator.
PAC-14028 is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.
Tivanisiran (SYL1001) is a siRNA used for the study of dry eye disease. Tivanisiran was designed to silence transient receptor potential vanilloid 1 (TRPV1)[1].
SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
TRPA1-IN-2 (compound 1) is a potent and orally active TRPA1 inhibitor with an IC50 value of 0.04 µM. TRPA1-IN-2 shows anti-inflammation activity[1].
Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM.
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).
SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM.
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].