Imarikiren
Product Specifications
CAS Number
1202265-63-1
Bioactivity
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 ?M) and cathepsin D (IC50 > 10 ?M) . 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.
Smiles
C(CCCOC)N1C(C(N(CC(C)C)[C@H]2C[C@@H](C(=O)N3CCOCC3)CNC2)=O)=NC=4C1=CC=CC4
Molecular Formula
C27H41N5O4
Molecular Weight
499.65
Shipping Conditions
Cool pack
Storage Temperature
-20°C
Available Sizes
Curated Selection
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