Aliskiren (hemifumarate)

Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].

Product Specifications

CAS Number

[173334-58-2]

Product Name Alternative

CGP 60536 (hemifumarate) ; CGP60536B (hemifumarate) ; SPP 100 (hemifumarate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Renin

Type

Reference compound

Related Pathways

Autophagy; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Aliskiren-hemifumarate.html

Purity

99.62

Solubility

H2O : ≥ 50 mg/mL

Smiles

O=C(O)/C=C/C(O)=O.O=C(NCC(C)(C(N)=O)C)[C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)CC1=CC=C(OC)C(OCCCOC)=C1)N)O)C(C)C.O=C(NCC(C)(C(N)=O)C)[C@H](C(C)C)C[C@H](O)[C@@H](N)C[C@@H](C(C)C)CC2=CC=C(OC)C(OCCCOC)=C2

Molecular Formula

C64H110N6O16

Molecular Weight

1219.59

Precautions

H302, H315, H319, H335

References & Citations

[1]Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754-758|[2]Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60 (5) :623-31.|[3]Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308 (4), 698-705.|[4]Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111 (8), 1012-1018.|[5]Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36 (5) :3014-3022. |[6]Ferri N, et al. Aliskiren inhibits prorenin-induced human aortic smooth muscle cell migration. J Renin Angiotensin Aldosterone Syst. 2015 Jun;16 (2) :284-91.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Citation 01

Department of Pharmaceutical Sciences. East Tennessee State University. 2015 May.|Drug Metab Pharmacokinet. 2024 Jun:56:101008.|Stanford University. 2025.|Toxicol Res Appl. 2018, 2:239784731880115.|Toxicol Res Appl. September 25, 2018.|Clin Sci. 2025 Jan 15;139 (1) :43-53.|Department of Biological Science. National Sun Yat-Sen University. 2015 Sep.|Front Biosci (Landmark Ed) . 2023 Oct 17;28 (10) :238.|Lipids Health Dis. 2018 Jul 31;17 (1) :183. |Neurobiol Dis. 2014 Nov;71:292-304.