Imarikiren HCl

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MedKoo CAT#: 526864

CAS#: 1202269-24-6 (HCl salt)

Description: 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.


Chemical Structure

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Imarikiren HCl
CAS# 1202269-24-6 (HCl salt)

Theoretical Analysis

MedKoo Cat#: 526864
Name: Imarikiren HCl
CAS#: 1202269-24-6 (HCl salt)
Chemical Formula: C27H42ClN5O4
Exact Mass:
Molecular Weight: 536.114
Elemental Analysis: C, 60.49; H, 7.90; Cl, 6.61; N, 13.06; O, 11.94

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: TAK-272; TAK 272; TAK272; TAK-272 hydrochloride; TAK-272 HCl. Imarikiren HCl |

IUPAC/Chemical Name: 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-yl)carbonylpiperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride

InChi Key: PUXOYQIZZIWCHH-NSLUPJTDSA-N

InChi Code: InChI=1S/C27H41N5O4.ClH/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;1H/t21-,22+;/m1./s1

SMILES Code: O=C(C1=NC2=CC=CC=C2N1CCCCOC)N(CC(C)C)[C@@H]3CNC[C@H](C(N4CCOCC4)=O)C3.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 536.114 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.

Recalculate based on batch purity %
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

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Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor Yasuhiro Imaeda, Hidekazu Tokuhara, Yoshiyuki Fukase, Ray Kanagawa, Yumiko Kajimoto, Keiji Kusumoto, Mitsuyo Kondo, Gyorgy Snell, Craig A. Behnke, and Takanobu Kuroita Publication Date (Web): September 12, 2016 (Letter) DOI: 10.1021/acsmedchemlett.6b00251



Additional Information

Related CAS#
1202265-63-1 (free base)
1202269-24-6 (HCl)

The aspartic proteinase renin is an attractive target for the treatment of hypertension and cardiovascular/renal disease such as chronic kidney disease and heart failure.