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

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

Cat. No.: HY-12177 Purity: 98.98%
Handling Instructions

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

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

Aliskiren hemifumarate Chemical Structure

Aliskiren hemifumarate Chemical Structure

CAS No. : 173334-58-2

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10 mM * 1 mL in Water USD 80 In-stock
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10 mg USD 60 In-stock
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50 mg USD 132 In-stock
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100 mg USD 216 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Aliskiren hemifumarate:

Top Publications Citing Use of Products

    Aliskiren hemifumarate 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 hemifumarate 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).
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    Description

    Aliskiren hemifumarate(CGP 60536 hemifumarate) 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

    1219.59

    Formula

    C₆₄H₁₁₀N₆O₁₆

    CAS No.

    173334-58-2

    SMILES

    O=C(O)/C=C/C(O)=O.O=C(NCC(C)(C(N)=O)C)[[email protected]@H](C[[email protected]@H]([[email protected]](C[[email protected]@H](C(C)C)CC1=CC=C(OC)C(OCCCOC)=C1)N)O)C(C)C.O=C(NCC(C)(C(N)=O)C)[[email protected]](C(C)C)C[[email protected]](O)[[email protected]@H](N)C[[email protected]@H](C(C)C)CC2=CC=C(OC)C(OCCCOC)=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 50 mg/mL (41.00 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8199 mL 4.0997 mL 8.1995 mL
    5 mM 0.1640 mL 0.8199 mL 1.6399 mL
    10 mM 0.0820 mL 0.4100 mL 0.8199 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
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    Keywords:

    Aliskiren hemifumarateCGP 60536 hemifumarateCGP60536B hemifumarateSPP 100 hemifumarateReninAutophagyInhibitorinhibitorinhibit

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