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Aliskiren hydrochloride

MCE China：Aliskiren hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-12176A

CAS：173399-03-6

Synonyms：CGP 60536 hydrochloride; CGP60536B hydrochloride; SPP 100 hydrochloride

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia-.

In Vitro：Aliskiren hydrochloride inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1]. Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2]. Aliskiren hydrochloride (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity[2].

In Vivo：Aliskiren hydrochloride (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets[3]. Aliskiren hydrochloride (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole‑body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting[4]. Aliskiren hydrochloride (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].

IC50 & Target：IC50: 1.5 nM (renin)[1]; 0.6 nM (human renin), 2 nM (marmoset renin), 80 nM (rat renin), 7 nM (dog renin), 11 nM (rabbit renin), 63 nM (guinea pig renin), 150 nM (pig renin)[2] In Vitro Aliskiren hydrochloride inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1]. Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2]. Aliskiren hydrochloride (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Aliskiren hydrochloride Related Antibodies Cell Migration Assay [2] Cell Line: Smooth muscle cell (SMC)

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References：

[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  [Content Brief]

[2]. 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.  [Content Brief]

[3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.  [Content Brief]

[4]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022.  [Content Brief]