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    Aliskiren Hemifumarate (CGP 60536)
    Aliskiren Hemifumarate (CGP 60536)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1771
    CAS #: 173334-58-2Purity ≥98%

    Description: Aliskiren hemifumarate (CGP-60536; CGP60536; Rasilez; SPP100; SPP-100; Tekturna), the hemifumarate salt form of Aliskiren, is a potent and direct renin inhibitor with antihypertensive activity. It inhibits renin with an IC50 of 1.5 nM. Aliskiren is the first-in-class drugs called direct renin inhibitors approved for use in the treatment of essential (primary) hypertension. 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. 

    References: Pharmacol Rep. 2008 Sep-Oct;60(5):623-31; Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.

    Related CAS #: 173334-57-1(free base)  

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    Molecular Weight (MW)609.83
    FormulaC30H53N3O6.1/2C4H4O4
    CAS No.173334-58-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (164.0 mM)
    Water: 100 mg/mL (164.0 mM)
    Ethanol: 100 mg/mL (164.0 mM)
    Other info

    Chemical Name: (αS,γS,δS,ζS)-δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-benzeneoctanamide, 2E-butenedioate

    InChi Key: KLRSDBSKUSSCGU-KRQUFFFQSA-N

    InChi Code: InChI=1S/2C30H53N3O6.C4H4O4/c2*1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36;5-3(6)1-2-4(7)8/h2*10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35);1-2H,(H,5,6)(H,7,8)

    SMILES Code: COC1=C(OCCCOC)C=C(C[[email protected]](C(C)C)C[[email protected]](N)[[email protected]@H](O)C[[email protected]](C(NCC(C)(C)C(N)=O)=O)C(C)C)C=C1.OC(/C=C/C(O)=O)=O

    Synonyms

    CGP060536B; SPP-100; CGP 060536B; SPP 100; CGP-060536B; Rasilez; SPP100; Tekturna


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    In Vitro

    In vitro activity: 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.  

    In VivoAliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets. Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension.
    Animal model
    Formulation & Dosage< 10 mg/kg, oral
    References

    Pharmacol Rep. 2008 Sep-Oct;60(5):623-31; Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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