136511-43-8

136511-43-8 structure

Name: SCH 42495
Chemical Name: N-[2(S)-(acetylhtiomethyl)-3-(2-methylphenyl)-1-oxopropyl]-L-methionine ethyl ester
CAS Number: 136511-43-8
Molecular Formula: C₂₀H₂₉NO₄S₂
Molecular Weight: 411.57900
Catalog: Signaling Pathways Metabolic Enzyme/Protease Neprilysin
Create Date: 2016-02-06 00:38:29
Modify Date: 2024-01-12 12:43:44
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].

Name	N-[2(S)-(acetylhtiomethyl)-3-(2-methylphenyl)-1-oxopropyl]-L-methionine ethyl ester
Synonyms	N-(2(S)-(ACETYLTHIOMETHYL)-3-(2-METHYLPHENYL)-1-OXOPROPYL)-L-METHIONINE ETHYL ESTER N-[2(S)-acetylthiomethyl-3-(2-methylphenyl)propionyl]-(S)-methionine ethyl ester

Description	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].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin
Target	NEP[1]
In Vitro	SCH 42354 selectively inhibits hydrolysis of leu-enkephalin and ANF (IC50 of 8.3 and 10.0 nM, respectively) in vitro[1].
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.
References	[1]. Watkins RW, et al. Atrial natriuretic factor potentiating and hemodynamic effects of SCH 42495, a new, neutral metalloendopeptidase inhibitor. Am J Hypertens. 1993 May;6(5 Pt 1):357-68. [2]. Thompson JS, et al. Effects of the neutral endopeptidase inhibitor, SCH 42495, on the cardiovascular remodelling secondary to chronic hypoxia in rats. Clin Sci (Lond). 1994 Jul;87(1):109-14.

Molecular Formula	C₂₀H₂₉NO₄S₂
Molecular Weight	411.57900
Exact Mass	411.15400
PSA	123.07000
LogP	3.62530

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