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145841-10-7

中文名稱 145841-10-7
英文名稱 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 結(jié)構(gòu)式 145841-10-7 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12866
英文別名
Sch-42495 (racemate)
L-Methionine, N-[2-[(acetylthio)methyl]-3-(2-methylphenyl)-1-oxopropyl]-, ethyl ester

物理化學(xué)性質(zhì)

沸點597.3±50.0 °C(Predicted)
密度1.158±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.50±0.46(Predicted)

常見問題列表

生物活性
SCH 42495 racemate 是 Sch-42495 的外消旋體。SCH 42495 是一種具有口服活性的中性金屬內(nèi)肽酶 (NEP) 抑制劑,具有抗高血壓活性。SCH 42495 是 SCH 42354 的口服活性前藥。
靶點

NEP

體外研究

SCH 42495 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC 50 of 8.3 and 10.0 nM, respectively) in vitro.

體內(nèi)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.
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