SA 57
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- CAS号:
- 1346169-63-8
- 英文名:
- SA 57
- 英文别名:
- SA 57;SA57,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
- 中文名:
- SA 57
- 中文别名:
- 化合物 T12826
- CBNumber:
- CB33037509
- 分子式:
- C17H23ClN2O3
- 分子量:
- 338.83
- MOL File:
- 1346169-63-8.mol
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SA 57化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 25 mM; Ethanol: 20 mM
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形态:
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A crystalline solid
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颜色:
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White to off-white
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SA 57性质、用途与生产工艺
SA57 是一种有效的选择性 FAAH 抑制剂，对小鼠和人类 FAAH 的 IC50 分别为 3.2 nM 和 1.9 nM。SA57 还抑制 2-花生四烯酸甘油水解酶 MAGL (对小鼠和人类 MAGL 的 IC50 分别为 410 nM 和 1.4 μM）和小鼠 α/β-水解酶结构域蛋白 6 (mABHD6; IC50 为 850 nM)，但不抑制其他脑丝氨酸水解酶。
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.
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Animal Model:
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C57Bl/6 mice
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Dosage:
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0.01 mg/kg, 0.05 mg/kg, 0.25 mg/kg, 1.25 mg/kg, 6.25 mg/kg, 12.5 mg/kg
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Administration:
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Intraperitoneal injection; for 2 hours
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Result:
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Showed distinct dose-responsive activity against brain serine hydrolases. Inhibited FAAH, MAGL and ABHD6 in vivo.
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SA 57
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/04/30 | HY-103463 | SA57 | | 1 mg | 670元 |
1346169-63-8, SA 57 相关搜索:
- 化合物 T12826
- 1346169-63-8
- SA57,SA-57
- 1-Piperidinecarboxylic acid, 4-[2-(4-chlorophenyl)ethyl]-, 2-(methylamino)-2-oxoethyl ester
- 4-[2-(4-Chlorophenyl)ethyl]-1-piperidinecarboxylic acid 2-(methylamino)-2-oxoethyl ester
- SA 57