TRPA1 Antagonist

PF-04745637 is a potent and selective TRPA1 antagonist with an IC₅₀ of 17 nM for human TRPA1.

GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma.

AMG2504 is a TRPA1 antagonist with an IC₅₀ value of 35 nM against human TRPA1. AMG2504 inhibits human TRPA1 activation induced by AITC and noxious cold stimulation. AMG2504 is applicable to research related to chronic pain.

Chembridge-5861528 (TCS 5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC₅₀ values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities.

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC₅₀ of 63.2 nM.

AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC₅₀ of 31.2 nM.

GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx.GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity.GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses.GRC-17536 exhibits antitussive activity.GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study.GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough.