AM0902检测

AM0902

用途靶点体外研究体内研究 用途与合成方法 MSDS AM0902价格(试剂级) 上下游产品信息中文名称中文同义词英文名称英文同义词CAS号分子式分子量EINECS号相关类别Mol文件结构式

AM0902

1-((3-(4-氯苯乙基)-1,2,4-恶二唑-5-基)甲基)-7-甲基-1H-嘌呤-6(7H)-酮;AM-0902游离;化合物AM-0902;AM 0902,TRPA1拮抗剂

AM-0902

AM0902;AM-0902;1-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-7-methylpurin-6-one;1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-purin-6-one;CS-2717;AM-0902 (AM 0902;6H-Purin-6-one, 1-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-;1-({3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl}methyl)-7-methyl-1,7-dihydro-6H-purin-6-one

1883711-97-4

C17H15ClN6O2

370.79

API

1883711-97-4.mol

AM0902 性质

熔点沸点密度储存条件溶解度酸度系数(pKa)形态颜色

190 - 197°C

657.3±65.0 °C(Predicted)

1.51±0.1 g/cm3(Predicted)

2-8°C

可溶于DMSO（轻微）、甲醇（非常轻微）

2.36±0.50(Predicted)

固体

白色至类白色

AM0902 用途与合成方法

用途

AM-0902是一种有效的、选择性的瞬时受体电位 A1 (TRPA1) 拮抗剂，作用于 rTRPA1 和 hTRPA1 的 IC50 值分别为 71 和 131 nM，已被证明在与疼痛相关的生物学途径中发挥重要作用。

靶点

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

体外研究

AM-0902 is a potent, selective antagonist of TRPA1 with IC 50 s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively. AM-0902 is highly permeable (average P app =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 45 Ca 2+ flux upon activation of rat TRPA1 with methylglyoxal with an IC 50 of 0.019 μM.

体内研究

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 45 Ca 2+ 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 45 Ca 2+ IC 50 , and unbound in vivo IC 90 of 1.7 μM are determined. It is noteworthy that at a dose of 30 mg/kg, AM-0902 engages TRPA1 at concentrations that exceed the in vivo IC 90 , making it a useful tool for exploration of in vivo models of acute pain.