1. Metabolic Enzyme/Protease
    Autophagy
  2. Renin
    Autophagy
  3. Aliskiren

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

Cat. No.: HY-12176 Purity: 99.16%
Handling Instructions

Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.

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

Aliskiren Chemical Structure

Aliskiren Chemical Structure

CAS No. : 173334-57-1

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10 mM * 1 mL in DMSO USD 102 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Aliskiren:

Top Publications Citing Use of Products

    Aliskiren purchased from MCE. 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.

    Aliskiren purchased from MCE. Usage Cited in: Lipids Health Dis. 2018 Jul 31;17(1):183.

    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).
    • Biological Activity

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    • Customer Review

    Description

    Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM. IC50 value: 1.5 nM [1] Target: renin in vitro: Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans [2]. in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4].

    Clinical Trial
    Molecular Weight

    551.76

    Formula

    C₃₀H₅₃N₃O₆

    CAS No.

    173334-57-1

    SMILES

    COCCCOC1=CC(C[[email protected]@H](C[[email protected]@H]([[email protected]](C[[email protected]](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
    Pure form -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (181.24 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8124 mL 9.0619 mL 18.1238 mL
    5 mM 0.3625 mL 1.8124 mL 3.6248 mL
    10 mM 0.1812 mL 0.9062 mL 1.8124 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.16%

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    Keywords:

    AliskirenCGP 60536CGP60536BSPP 100CGP60536CGP-60536SPP100SPP-100ReninAutophagyInhibitorinhibitorinhibit

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    Cat. No.:
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