136511-43-8
136511-43-8 結(jié)構(gòu)式
基本信息
英文別名
SCH 42495ETHYL 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
物理化學(xué)性質(zhì)
沸點597.3±50.0 °C(Predicted)
密度1.158±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)13.50±0.46(Predicted)
常見問題列表
生物活性
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 42354 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. |