1202265-63-1
Chemical Structure
Imarikiren
Synonym(s): AK-272 free base; SCO-272 free base
- CAS No.: 1202265-63-1
- Formula:C27H41N5O4
- Molecular Weight:499.65
IUPAC Name: N-isobutyl-1-(4-methoxybutyl)-N-((3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl)-1H-benzo[d]imidazole-2-carboxamide
InChIKey: RHIBAIKQWJNESW-YADHBBJMSA-N
SMILES: COCCCCN1C(C(N([C@H]2C[C@H](CNC2)C(N3CCOCC3)=O)CC(C)C)=O)=NC4=CC=CC=C41
Biological Activity: Imarikiren (AK-272 free base) is an orally active, selective Renin inhibitor with an IC50 value of 2.1 nM against h-Renin. Imarikiren blocks the conversion of Angiotensinogen to Angiotensin I and reduces mean arterial pressure by inhibiting Angiotensin II that binds to AT1. Imarikiren alleviates myocardial hypertrophy and pulmonary congestion, exerting cardioprotective effects. Imarikiren can be used in research related to hypertension and heart failure[1][2][3].
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Imarikiren | Imarikiren (AK-272 free base) is an orally active, selective Renin inhibitor with an IC50 value of 2.1 nM against h-Renin. Imarikiren blocks the conversion of Angiotensinogen to Angiotensin I and reduces mean arterial pressure by inhibiting Angiotensin II that binds to AT1. Imarikiren alleviates myocardial hypertrophy and pulmonary congestion, exerting cardioprotective effects. Imarikiren can be used in research related to hypertension and heart failure. | |||||||||||||||||||||
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- [1]. Imaeda Y, et al. Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor. ACS medicinal chemistry letters. 2016 Oct 13;7(10):933-938. [Content Brief]
- [2]. Hara T, et al. TAK-272 (imarikiren), a novel renin inhibitor, improves cardiac remodeling and mortality in a murine heart failure model. PloS one. 2018;13(8):e0202176. [Content Brief]
- [3]. Gebremichael Y, et al. Benchmarking renin suppression and blood pressure reduction of direct renin inhibitor imarikiren through quantitative systems pharmacology modeling. Journal of pharmacokinetics and pharmacodynamics. 2019 Feb;46(1):15-25. [Content Brief]
Keywords
