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.
