Imarikiren, also known as TAK-272, is a potent, selective and orally active direct renin inhibitor for the treatment of diabetic nephropathies. TAK-272 showed potent inhibitory activity against human renin (IC50 = 2.1 nM) in hPRA assay and excellent selectivity against other aspartic proteases, such as pepsin (IC50 > 10 μM) and cathepsin D (IC50 > 10 μM). TAK-272 exhibited a dramatically improved PK profile in rats (F = 25.2%). TAK-272 (3 and 10 mg/kg, p.o.) exhibited potent and long-lasting antihypertensive efficacy in a dose-dependent manner. TAK-272 HCl is currently undergoing human clinical trials.
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名称 | Imarikiren |
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Iupac 化学名称 | N-isobutyl-1-(4-methoxybutyl)-N-((3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl)-1H-benzo[d]imidazole-2-carboxamide |
同义词 | IMARIKIREN; TAK-272 free base; TAK-272 free base, (+)-; 01IC75R817; 1202265-63-1 |
英文同义词 | IMARIKIREN; TAK-272 free base; TAK-272 free base, (+)-; 01IC75R817; 1202265-63-1 |
分子式 | C27H41N5O4 |
分子量 | 499.65 |
Smile | COCCCCN1C2=CC=CC=C2N=C1C(=O)N(CC(C)C)[C@@H]3CNC[C@@H](C3)C(=O)N4CCOCC4 |
InChiKey | RHIBAIKQWJNESW-YADHBBJMSA-N |
InChi | InChI=1S/C27H41N5O4/c1-20(2)19-32(22-16-21(17-28-18-22)26(33)30-11-14-36-15-12-30)27(34)25-29-23-8-4-5-9-24(23)31(25)10-6-7-13-35-3/h4-5,8-9,20-22,28H,6-7,10-19H2,1-3H3/t21-,22+/m1/s1 |
Cas号 | 1202265-63-1 |
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