2. Metabolic Enzyme/Protease Autophagy
  3. Renin Autophagy
  4. Aliskiren hydrochloride

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

Cat. No.: HY-12176A
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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

Aliskiren hydrochloride Chemical Structure

CAS No. : 173399-03-6

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Aliskiren hydrochloride Related Antibodies

Top Publications Citing Use of Products

    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

    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[1]-[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.

    Aliskiren hydrochloride Related Antibodies

    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.
    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
    References
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    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.

    Keywords:

    Aliskiren173399-03-6CGP 60536CGP60536BSPP 100CGP60536CGP-60536SPP100SPP-100ReninAutophagyHypertensioncardiovascular diseasescancercachexiaC26colon carcinomaInhibitorinhibitorinhibit

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