Aliskiren hydrochloride (Synonyms: CGP 60536 hydrochloride; CGP60536B hydrochloride; SPP 100 hydrochloride)

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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^-.

For research use only. We do not sell to patients.

Aliskiren hydrochloride Chemical Structure

CAS No. : 173399-03-6

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Other In-stock Forms of Aliskiren hydrochloride:

Aliskiren Aliskiren hemifumarate

Other Forms of Aliskiren hydrochloride:

8 Publications Citing Use of MCE Aliskiren hydrochloride

: Aliskiren hydrochloride purchased from MedChemExpress. Usage Cited in: Lipids Health Dis. 2018 Jul 31;17(1):183. [Abstract]; Protein abundance of ER stress markers (BiP, IRE1α, PERK, ATF4, pS51-eIF2α, eIF2α, and CHOP) are upregulated after palmitic acid (PA) treatment, which is prevented by cotreatment with chymostatin (50μM) and Aliskiren (10 nM).

: Aliskiren hydrochloride purchased from MedChemExpress. Usage Cited in: Department of Biological Science. National Sun Yat-Sen University. 2015 Sep.; Effects of Aliskiren (AK) produce efficacious antagonism of the protein expression of c-Fos (A), GFAP (B) and OX-42 (C) in SC, aCSF+MCAO, AK+MCAO or AK alone group one day after stroke.

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Description

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.

Cell Migration Assay ^[2]

Cell Line:	Smooth muscle cell (SMC)
Concentration:	1-10 μM
Incubation Time:	24 hours
Result:	Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Sodium-depleted marmosets^[3]
Dosage:	3 mg/kg, 10 mg/kg
Administration:	Oral gavage; once daily; 12 days
Result:	Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate. Showed no rebound increase in BP following the end of treatment with either dose of aliskiren. Inhibited the RAS and controls the upregulation of pro‑inflammatory cytokines.

Animal Model:	Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells^[4]
Dosage:	10 mg/kg
Administration:	Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection
Result:	Enhanced grip strength, coordination, and locomotor activity. Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor‑α (TNF‑α) and inter‑ leukin‑6 (IL‑6) levels.

Clinical Trial

Molecular Weight

588.22

Formula

C₃₀H₅₄ClN₃O₆

CAS No.

173399-03-6

SMILES

[H]Cl.COCCCOC1=CC(C[C@@H](C[C@@H]([C@H](C[C@H](C(NCC(C)(C(N)=O)C)=O)C(C)C)O)N)C(C)C)=CC=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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]

Aliskiren hydrochloride Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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