Aliskiren

• CAT Number: I002255
• CAS Number: 173334-57-1
• Molecular Formula: C30H53N3O6
• Molecular Weight: 551.77
• Purity: ≥95%
• Target: Renin
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 1.5 nM
• InChI: InChI=1S/C30H53N3O6/c1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36/h10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35)/t22-,23-,24-,25-/m0/s1
• InChIKey: UXOWGYHJODZGMF-QORCZRPOSA-N
• SMILES: COCCCOC1=C(OC)C=CC(C[C@@H](C[C@H](N)[C@@H](O)C[C@@H](C(C)C)C(=O)NCC(C)(C)C(N)=O)C(C)C)=C1

Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM. Aliskiren is the first in a class of drugs called direct renin inhibitors. Its current licensed indication is essential (primary) hypertension. While used for high blood pressure, other better studied medications are typically recommended due to concerns of higher side effects and less evidence of benefit. In December 2011, Novartis halted a clinical trial of the drug after discovering increased incidence of nonfatal stroke, kidney complications, high blood potassium, and low blood pressure in people with diabetes and kidney impairment.

Reference

1: Zheng SL, Roddick AJ, Ayis S. Effects of aliskiren on mortality,
cardiovascular outcomes and adverse events in patients with diabetes and
cardiovascular disease or risk: A systematic review and meta-analysis of 13,395
patients. Diab Vasc Dis Res. 2017 Sep;14(5):400-406. doi:
10.1177/1479164117715854. Epub 2017 Aug 27. Review. PubMed PMID: 28844155; PubMed
Central PMCID: PMC5600262.

2: Nadeem S, Batisky DL. Aliskiren, the first direct renin inhibitor: assessing a
role in pediatric hypertension and kidney diseases. Pediatr Nephrol. 2014
Nov;29(11):2105-11. doi: 10.1007/s00467-013-2716-0. Epub 2013 Dec 14. Review.
PubMed PMID: 24337365; PubMed Central PMCID: PMC4057986.

3: Friedrich S, Schmieder RE. Review of direct renin inhibition by aliskiren. J
Renin Angiotensin Aldosterone Syst. 2013 Sep;14(3):193-6. doi:
10.1177/1470320313497328. Epub 2013 Jul 19. Review. PubMed PMID: 23873285.

4: Rashikh A, Ahmad SJ, Pillai KK, Najmi AK. Aliskiren as a novel therapeutic
agent for hypertension and cardio-renal diseases. J Pharm Pharmacol. 2012
Apr;64(4):470-81. doi: 10.1111/j.2042-7158.2011.01414.x. Epub 2011 Dec 7. Review.
PubMed PMID: 22420653.