SCH 42495
| 中文名称 | SCH 42495 |
|---|---|
| 中文同义词 | 化合物 T12641L;化合物 SCH 42495 |
| 英文名称 | SCH 42495 |
| 英文同义词 | 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 |
| CAS号 | 136511-43-8 |
| 分子式 | C20H29NO4S2 |
| 分子量 | 411.58 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 136511-43-8.mol |
| 结构式 |  |
SCH 42495 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) |
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。
NEP
SCH 42354 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC 50 of 8.3 and 10.0 nM, respectively) in vitro.
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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