A nonpeptide renin inhibitor
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Aliskiren (hemifumarate)

Item No. 19640

Technical Information
Formal 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
CAS Number
173334-58-2
Synonyms
  • CGP 60536
  • SPP 100
Molecular Formula
C30H53N3O6 • 1/2C4H4O4
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMSO: 100 mg/mLEthanol: 100 mg/mLWater: 100 mg/mL
λmax
280 nm
SMILES
COC1=C(OCCCOC)C=C(C[C@H](C(C)C)C[C@H](N)[C@@H](O)C[C@H](C(NCC(C)(C)C(N)=O)=O)C(C)C)C=C1.OC(/C=C/C(O)=O)=O
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)
InChi Key
KLRSDBSKUSSCGU-KRQUFFFQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Aliskiren is a nonpeptide inhibitor of renin (IC50 = 0.6 nM for the human enzyme).1 Aliskiren (10 and 30 mg/kg per day) reduces blood pressure and prevents albuminuria in renin-overexpressing TG(mRen-2)27 rats in a model of streptozotocin-induced diabetes.2 It also reduces cardiac hypertrophy and fibrosis induced by heart pressure overload in mice.3 Formulations containing aliskiren have been used in the treatment of hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rhuel, R., Rasetti, V., Maibaum, J., et alStructure-based drug design: The discovery of novel nonpeptide orally active inhibitors of human renin. Chem. Biol. 7(7), 493-504 (2000).

    2. Feldman, D.L., Jin, L., Xuan, H., et alEffects of aliskiren on blood pressure, albuminuria, and (pro)renin receptor expression in diabetic TG(mRen-2)27 rats. Hypertension 52(1), 130-136 (2008).

    3. Weng, L., Zhang, W., Ye, Y., et alAliskiren ameliorates pressure overload-induced heart hypertrophy and fibrosis in mice. Acta Pharmacol. Sin. 35(8), 1005-1014 (2014).