Biochem/physiol Actions
AM-0902 (AMG0902) is a potent and selective transient receptor potential A1 (TRPA1) antagonist (rat/human TRPA1 IC50 = 71/131 nM against AITC-induced 45Ca2+ influx in respective CHO transfectants with [AITC] = EC90 = 3 μM/hTRPA1 or 35 μM/rTRPA1; human/rat IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4, human CYP3A4/2D6, rat TRPV1/3, rat TRPM8, or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a rat pain model (by 65% and 85%, respectively, with 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic properties, oral availability and brain exposure (F = 60%, B/P = 0.2; 30 mg/kg p.o. in rats) in vivo.
- UPC:
- 51372301
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- SML2985-25MG
- CAS:
- 1883711-97-4