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
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(diǎn)597.3±50.0 °C(Predicted)
密度1.158±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)13.50±0.46(Predicted)
常見(jiàn)問(wèn)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(diǎn)
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. |