SA 57
中文名称 | SA 57 |
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中文同义词 | 化合物 T12826 |
英文名称 | SA 57 |
英文同义词 | SA 57;4-[2-(4-Chlorophenyl)ethyl]-1-piperidinecarboxylic acid 2-(methylamino)-2-oxoethyl ester;1-Piperidinecarboxylic acid, 4-[2-(4-chlorophenyl)ethyl]-, 2-(methylamino)-2-oxoethyl ester;SA57,SA-57 |
CAS号 | 1346169-63-8 |
分子式 | C17H23ClN2O3 |
分子量 | 338.83 |
EINECS号 | |
相关类别 | |
Mol文件 | 1346169-63-8.mol |
结构式 |
SA 57 性质
储存条件 | Store at -20°C |
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溶解度 | 二甲基亚砜:25mM;乙醇:20 mM |
形态 | 结晶固体 |
颜色 | 白色至米白色 |
IC50: 3.2 nM (Mouse FAAH) and 1.9 nM (Human FAAH); 410 nM (Mouse MAGL) and 1.4 μM (Human MAGL); 850 nM (Mouse ABHD6)
O-Aryl carbamate and N-aryl urea inhibitors have been shown to irreversibly inhibit FAAH by carbamylation of the enzyme’s serine nucleophile. SA57 exhibits clear time-dependent inhibition of FAAH and MAGL, suggesting a covalent mechanism of inactivation, presumably through carbamylation of the active site serine nucleophiles of these enzymes.
SA57 (0.01-12.5 mg/kg; intraperitoneal injection; for 2 hours; C57Bl/6 mice) treatment shows distinct dose-responsive activity against brain serine hydrolases (FAAH, MAGL and ABHD6) in vivo.
Animal Model: | C57Bl/6 mice |
Dosage: | 0.01 mg/kg, 0.05 mg/kg, 0.25 mg/kg, 1.25 mg/kg, 6.25 mg/kg, 12.5 mg/kg |
Administration: | Intraperitoneal injection; for 2 hours |
Result: | Showed distinct dose-responsive activity against brain serine hydrolases. Inhibited FAAH, MAGL and ABHD6 in vivo. |