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Aliskiren | direct renin inhibitor

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Price:
$159.00
Catalog #:
C2547-5
Quantity:


Product Description

Aliskiren is an orally-available, nonpeptide piperidine-based inhibitor renin (IC50 0.6 nM) for the treatment of hypertension. [1] Despite it's 2.5% bioavailability in humans, the absorbed aliskiren is slowly cleared such that the drug can accumulate to therapeutic levels within several doses.

Aliskiren is highly selective for the Renin-Angiotensin System (RAS) and therefore does not interfere with bradykinin metabolism; therefore side effects often associated with ACE inhibitors are not likely to occur with aliskiren. [2] Aliskiren is effective in reducing blood pressure and is well tolerated, and has shown promising target organ protection in animal models and clinical trials. [3]


Technical information:

Chemical Formula:   C30H53N3O6
CAS #:   173334-57-1, 173334-58-2
Molecular Weight:   551.76
Purity:   >98%
Appearance:   White
Chemical Name:   (2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide
Solubility:   Up to 22 mM in DMSO
Synonyms:   Aliskiren, Rasilez, Tekturna, CGP60536B

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Brown, M.J., Aliskiren. Circulation, 2008, 118, 773-784. Pubmed ID: 18695203
2. Allikmets, K., Aliskiren--an orally active renin inhibitor. Review of pharmacology, pharmacodynamics, kinetics, and clinical potential in the treatment of hypertension.Vasc. Heatlh Risk Mgmt., 2007, 3(6), 809-815. Pubmed ID: 18200801
3. Gradman et al., Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation 2005, 111, 1012-1018. Pubmed ID: 15723979

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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