1202269-24-6
Chemical Structure
Imarikiren hydrochloride
Synonym(s): AK-272; SCO-272
- CAS No.: 1202269-24-6
- Formula:C27H42ClN5O4
- Molecular Weight:536.11
IUPAC Name: N-isobutyl-1-(4-methoxybutyl)-N-((3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl)-1H-benzo[d]imidazole-2-carboxamide hydrochloride
InChIKey: PUXOYQIZZIWCHH-NSLUPJTDSA-N
SMILES: COCCCCN1C(C(N([C@H]2C[C@H](CNC2)C(N3CCOCC3)=O)CC(C)C)=O)=NC4=CC=CC=C14.Cl
Biological Activity: Imarikiren hydrochloride (AK-272) is an orally active, selective Renin inhibitor with an IC50 value of 2.1 nM against h-Renin. Imarikiren hydrochloride blocks the conversion of Angiotensinogen to Angiotensin I and reduces mean arterial pressure by inhibiting Angiotensin II that binds to AT1. Imarikiren hydrochloride alleviates myocardial hypertrophy and pulmonary congestion, exerting cardioprotective effects. Imarikiren hydrochloride can be used in research related to hypertension and heart failure[1][2][3].
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Imarikiren hydrochloride | Imarikiren hydrochloride (AK-272) is an orally active, selective Renin inhibitor with an IC50 value of 2.1 nM against h-Renin. Imarikiren hydrochloride blocks the conversion of Angiotensinogen to Angiotensin I and reduces mean arterial pressure by inhibiting Angiotensin II that binds to AT1. Imarikiren hydrochloride alleviates myocardial hypertrophy and pulmonary congestion, exerting cardioprotective effects. Imarikiren hydrochloride can be used in research related to hypertension and heart failure. | |||||||||||||||||||||
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References
- [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]
