113082-98-7

113082-98-7 structure

Name: Enalkiren
Chemical Name: 3-amino-N-[(2S)-1-[[(2S)-1-[[(2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-3-methylbutanamide
CAS Number: 113082-98-7
Molecular Formula: C₃₅H₅₆N₆O₆
Molecular Weight: 656.85600
Catalog: Signaling Pathways Metabolic Enzyme/Protease Renin
Create Date: 2018-05-06 08:00:00
Modify Date: 2024-01-06 19:27:41
Enalkiren (A-64662) is a potent dipeptide renin inhibitor with an IC50 of 0.78 nM in a purified renal renin-angiotensinogen system (pH=6.0). Enalkiren suppresses renin activity, and also reduces systolic and diastolic blood pressure. Enalkiren can be used to research essential hypertension[1][2].

Name	3-amino-N-[(2S)-1-[[(2S)-1-[[(2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-3-methylbutanamide
Synonyms	Enalquireno [INN-Spanish] Enalkirene [INN-French] ENALKIREN Enalkirenum [INN-Latin] Enalquireno L-Histidinamide,N-(3-amino-3-methyl-1-oxobutyl)-O-methyl-L-tyrosyl-N-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-,(1S-(1R,2S,3R*))

Description	Enalkiren (A-64662) is a potent dipeptide renin inhibitor with an IC50 of 0.78 nM in a purified renal renin-angiotensinogen system (pH=6.0). Enalkiren suppresses renin activity, and also reduces systolic and diastolic blood pressure. Enalkiren can be used to research essential hypertension[1][2].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Metabolic Enzyme/Protease >> Renin
Target	IC50: 23 nM (hamster dipeptide renin), 14 nM (human dipeptide renin), 2.3 nM (cynomolgus monkey dipeptide renin)[2]
In Vitro	Enalkiren inhibits the endogenous renin-angiotensinogen reaction with an IC50 value of 23 nM, 14 nM and 2.3 nM in hamster, human and cynomolgus monkey plasma, respectively, at pH 7.4[2].
In Vivo	Enalkiren (0.01-10 mg/kg; i.v.; single dosage) reduces mean arterial blood pressure in cynomolgus monkey[2]. Animal Model: Cynomolgus monkey[2] Dosage: 0.01-10 mg/kg Administration: i.v.; single dosage Result: Reduced mean arterial blood pressure in a dose-related manner.