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Enalkiren

Names

[ CAS No. ]:
113082-98-7

[ Name ]:
Enalkiren

[Synonym ]:
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*))

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.172g/cm3

[ Boiling Point ]:
986.3ºC at 760mmHg

[ Molecular Formula ]:
C35H56N6O6

[ Molecular Weight ]:
656.85600

[ Flash Point ]:
550.3ºC

[ Exact Mass ]:
656.42600

[ PSA ]:
191.69000

[ LogP ]:
4.39660

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.559

Related Compounds