1346169-63-8
1346169-63-8 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12826 英文別名
SA 57SA57,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
物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 25 mM; Ethanol: 20 mM
形態(tài)結(jié)晶固體
顏色White to off-white
常見問題列表
生物活性
SA57 是一種有效的選擇性 FAAH 抑制劑，對(duì)小鼠和人類 FAAH 的 IC50 分別為 3.2 nM 和 1.9 nM。SA57 還抑制 2-花生四烯酸甘油水解酶 MAGL (對(duì)小鼠和人類 MAGL 的 IC50 分別為 410 nM 和 1.4 μM）和小鼠 α/β-水解酶結(jié)構(gòu)域蛋白 6 (mABHD6; IC50 為 850 nM)，但不抑制其他腦絲氨酸水解酶。靶點(diǎn)
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)
體外研究
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.
體內(nèi)研究
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. |