Aliskiren hydrochloride
Based on 11 publication(s) in Google Scholar
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-.
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- CAS No.: 173399-03-6
- Formule: C30H54ClN3O6
- Masse moléculaire:588.22
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Aliskiren hydrochloride
More- Clin Sci. 2025 Jan 15;139(1):43-53. [Abstract]
- Lipids Health Dis. 2018 Jul 31;17(1):183. [Abstract]
- Biochem Pharmacol. 2026 Mar:245:117635. [Abstract]
- Neurobiol Dis. 2014 Nov:71:292-304. [Abstract]
- Front Biosci (Landmark Ed). 2023 Oct 17;28(10):238. [Abstract]
- Drug Metab Pharmacokinet. 2024 Jun:56:101008. [Abstract]
- Stanford University. 2025.
- Toxicol Res Appl. 2018, 2:239784731880115.
- Toxicol Res Appl. September 25, 2018.
- National Sun Yat-Sen University. 2015 Sep.
- East Tennessee State University. 2015 May.
Customer Validation & Images
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Activité biologique
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]
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.
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Cell Line:Smooth muscle cell (SMC)
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Concentration:1-10 μM
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Incubation Time:24 hours
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Result:Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.
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.
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Animal Model:Sodium-depleted marmosets[3]
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Dosage:3 mg/kg, 10 mg/kg
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Administration:Oral gavage; once daily; 12 days
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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.
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Animal Model:Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells[4]
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Dosage:10 mg/kg
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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
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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.
Chemical Information
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CAS No. 173399-03-6
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Masse moléculaire 588.22
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Formule C30H54ClN3O6
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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
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Synonyms
CGP 60536 hydrochloride; CGP60536B hydrochloride; SPP 100 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (11)
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Journal Impact Factor
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Most Recent
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Clin Sci
Higher circulating ACE2 and DPP3 but reduced ACE and angiotensinogen in hyperreninemic sepsis patients. [Abstract]2025 Jan 15;139(1):43-53. PMID: 39699964 -
Lipids Health Dis
Combination of Chymostatin and Aliskiren attenuates ER stress induced by lipid overload in kidney tubular cells. [Abstract]2018 Jul 31;17(1):183. PMID: 30064425
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).
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Biochem Pharmacol
Renin inhibition improved muscular function by alleviating insulin resistance and AGEs/RAGE signaling in skeletal muscle associated with high glucose: Exploration of renin inhibitor tanshinone IIA. [Abstract]2026 Mar:245:117635. PMID: 41391695 -
Neurobiol Dis
Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. [Abstract]2014 Nov:71:292-304. PMID: 25131447 -
Front Biosci (Landmark Ed)
C3aR Antagonist Alleviates C3a Induced Tubular Profibrotic Phenotype Transition via Restoring PPARα/CPT-1α Mediated Mitochondrial Fatty Acid Oxidation in Renin-Dependent Hypertension. [Abstract]2023 Oct 17;28(10):238. PMID: 37919077 -
Drug Metab Pharmacokinet
2024 Jun:56:101008. PMID: 38663183 -
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Aliskiren hydrochloride purchased from MedChemExpress. Usage Cited in: 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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Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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