Name: Imarikiren
Rating: 4 (6 reviews)

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HIT ID:HIT218695998
Cas No:1202265-63-1
Common Name:Imarikiren
alias:TAK-272 free base, (+)-, TAK-272 free base, 01IC75R817
alias:TAK-272 free base, (+)-, TAK-272 free base, 01IC75R817
IUPAC:1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl]-1H-1,3-benzodiazole-2-carboxamide
IUPAC:1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl]-1H-1,3-benzodiazole-2-carboxamide
InChIKey:RHIBAIKQWJNESW-YADHBBJMSA-N

Molecular Formula:C27H41N5O4
Molecular Weight:499.656
Hydrogen Bond Donor (HBD):
Hydrogen Bond Acceptor (HBA):
LogP:
SMILES:COCCCCn1c(nc2ccccc12)C(=O)N(CC(C)C)[C@@H]1CNC[C@@H](C1)C(=O)N1CCOCC1
SMILES:COCCCCn1c(nc2ccccc12)C(=O)N(CC(C)C)[C@@H]1CNC[C@@H](C1)C(=O)N1CCOCC1

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC₅₀ = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC₅₀ > 10 μM) and cathepsin D (IC₅₀ > 10 μM). In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg/kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.

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