Imarikiren HCl

TargetMol
Product Code: TAR-T27595
Supplier: TargetMol
CodeSizePrice
TAR-T27595-5mg5mg£1,091.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
TAR-T27595-50mg50mg£2,143.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
TAR-T27595-100mg100mg£2,801.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

1 / 1

Further Information

Bioactivity:
Imarikiren is a potent, selective and orally active direct renin inhibitor. TAK-272 shows potent inhibitory activity against human renin (IC50 = 2.1 nM) in hPRA assay and excellent selectivity against other aspartic proteases, such as cathepsin D (IC50 > 10 μM) and pepsin (IC50 > 10 μM). TAK-272 exhibits a dramatically improved PK profile in rats (F = 25.2%). TAK-272 (3 and 10 mg/kg, p.o.) exhibits potent and long-lasting antihypertensive efficacy in a dose-dependent manner.
CAS:
1202269-24-6
Formula:
C27H42ClN5O4
Molecular Weight:
536.11
Purity:
0.98
SMILES:
Cl.COCCCCn1c(nc2ccccc12)C(=O)N(CC(C)C)[C@@H]1CNC[C@@H](C1)C(=O)N1CCOCC1

References

1. 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