AM-0902 是一种有效的选择性瞬时受体电位 A1 (TRPA1) 拮抗剂，作用于 rTRPA1 和 hTRPA1 的 IC₅₀ 值分别为 71 和 131 nM。

AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC 50 s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.

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IC50: 71 nM (rTRPA1), 131 nM (hTRPA1)

AM-0902 is a potent, selective antagonist of TRPA1 with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively. AM-0902 is highly permeable (average Papp=44.5 μcm/s in MDCK cells), an unlikely substrate for P-gp (efflux ratio=1.3 in P-gp overexpressing MDCK cells), and demonstrates good solubility (PBS pH 7.4: 226 μM, SIF: 248 μM). AM-0902 shows good selectivity over other TRP channels, as no activity is observed against human TRPV1 or TRPV4, or rat TRPV1, TRPV3, or TRPM8, at concentrations up to 10 μM. AM-0902 inhibits Ca flux upon activation of rat TRPA1 with methylglyoxal with an IC50 of 0.019 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

AM-0902 is a potent, selective antagonist of TRPA1 in vivo. AM-0902 has moderate terminal elimination half-life (t 1/2 =0.6 h and 2.8 h for rat (0.5 mg/kg, iv), rat (30 mg/kg, oral)). A dose-dependent reduction of allyl isothiocyanate (AITC)-induced flinching is observed for AM-0902, with a significant reduction in flinching observed postdosing of 10 and 30 mg/kg. The unbound plasma concentrations (C u ) at 1 h for the 1, 3, 10, and 30 mg/kg doses are 0.051±0.024 (n=8), 0.19±0.11 (n=8), 0.58±0.35 (n=8), and 2.2±0.40 (n=8) μM, covering the in vitro rat TRPA1 Ca IC 50 at 0.72, 2.7, 8.2, and 30.3 fold, respectively. A good exposure-response relationship is observed in this target coverage model. An unbound in vivo IC 50 of 0.35 μM, which is in good agreement with the in vitro rat TRPA1 Ca IC 50 , and unbound in vivo IC 90 o

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[1]. Schenkel LB, et al. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1)Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809.

In Vitro: DMSO : 150 mg/mL (404.54 mM; Need ultrasonic and warming)配制储备液