145841-10-7
中文名称
145841-10-7
英文名称
Sch-42495 (racemate)
CAS
145841-10-7
分子式
C20H29NO4S2
分子量
411.58
MOL 文件
145841-10-7.mol
145841-10-7 结构式
基本信息
中文别名
化合物 T12866 英文别名
Sch-42495 (racemate)L-Methionine, N-[2-[(acetylthio)methyl]-3-(2-methylphenyl)-1-oxopropyl]-, ethyl ester
物理化学性质
沸点597.3±50.0 °C(Predicted)
密度1.158±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)13.50±0.46(Predicted)
常见问题列表
生物活性
SCH 42495 racemate 是 Sch-42495 的外消旋体。SCH 42495 是一种具有口服活性的中性金属内肽酶 (NEP) 抑制剂，具有抗高血压活性。SCH 42495 是 SCH 42354 的口服活性前药。靶点
NEP
体外研究
SCH 42495 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC 50 of 8.3 and 10.0 nM, respectively) in vitro.
体内研究
SCH 42495 (30 mg/kg; oral gavage; twice daily) causes a significant reduction in the pulmonary vascular remodelling and ventricular hypertrophy in hypoxic rats after 10 days.
Treatment with SCH 42495 (30 mg/kg; oral gavage; twice daily) leads to a decrease in cardiovascular remodelling secondary to chronic hypoxia in rats.
SCH 42495 (oral doses of 1, 3, or 10 mg/kg) produces significant reductions in blood pressure in DOCA-N a hypertensive rats of 22±6, 43±7, and 62±12 mm Hg, respectively.
| Animal Model: | Hypoxic rats |
| Dosage: | 30 mg/kg |
| Administration: | Oral gavage; twice daily for 10 days |
| Result: |
Caused a significant reduction in the pulmonary vascular remodelling and ventricular hypertrophy.
Led to a decrease in cardiovascular remodelling secondary to chronic hypoxia. |