TRP Channel Antagonist

Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC₅₀ of 562 nM.

HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively.

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC₅₀s of 2 nM and 40 nM for rTRPV4 and hTRPV4.

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.

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.

AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC₅₀ of 0.5 nM.

A-967079 is a selective TRPA1 receptor antagonist with IC₅₀s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the blood-brain barrier.

BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC₅₀s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.

SET2 is a selective TRPV2 antagonist (IC₅₀=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases.

GSK205 is a potent, selective TRPV4 antagonist with an IC₅₀ of 4.19  μM for inhibiting TRPV4-mediated Ca²⁺ influx.

SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC₅₀ of 7.1.

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.

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.

RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC₅₀s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.

HC-070 is an antagonist of TRPC4/TRPC5, with IC₅₀s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.

Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (K_i=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca²⁺ influx with an IC₅₀ value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain.

SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC₅₀ value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity.

(E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC₅₀ of 454 nM.

PF-05105679, a chemical probe, is an orally active and selective TRPM8 antagonist with an IC₅₀ of 103 nM. PF-05105679 has the potential for cold-related pain.

Ononetin, a natural deoxybenzoin, is a potent and selective TRPM3 channel blocker with an IC₅₀ of 0.3 μM.