Sch 42495

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Sch 42495

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

136511-43-8

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。

生物活性

SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354^[1].

IC₅₀& Target

NEP^[1]

体外研究
(In Vitro)

SCH 42354 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC₅₀of 8.3 and 10.0 nM, respectively) in vitro^[1].

体内研究
(In Vivo)

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^[2].
Treatment with SCH 42495 (30 mg/kg; oral gavage; twice daily) leads to a decrease in cardiovascular remodelling secondary to chronic hypoxia in rats^[2].
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^[1].

Animal Model:	Hypoxic rats^[2]
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.

分子量

411.58

Formula

C₂₀H₂₉NO₄S₂

CAS 号

136511-43-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.