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.
MedKoo Cat#: 125540
Name: Imarikiren
CAS#: 1202265-63-1 (free base)
Chemical Formula: C27H41N5O4
Exact Mass: 499.3200
Molecular Weight: 499.66
Elemental Analysis: C, 64.90; H, 8.27; N, 14.02; O, 12.81
The following data is based on the product molecular weight 499.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
