136511-43-8

中文名称 SCH 42495

CAS 136511-43-8

分子式 C20H29NO4S2

分子量 411.58

MOL 文件 136511-43-8.mol

136511-43-8 结构式

基本信息物理化学性质常见问题列表

基本信息

英文别名

SCH 42495
ETHYL N-{2-[(ACETYLTHIO)METHYL]-3-(O-TOLYL)-1-OXOPROPYL}-L-METHIONATE
N-(2(S)-(Acetylthiomethyl)-3-(2-Methylphenyl)-1- Oxopropyl)-L-Methionine Ethyl Ester
L-Methionine, N-[(2S)-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)

酸度系数(pKa)13.50±0.46(Predicted)

常见问题列表

生物活性

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 42354 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.