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Product Description
Aliskiren hemifumarate(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].
Information
CAS No173334-58-2
FormulaC64H110N6O16
Clinical Informationclinicalinformation
PathwayMetabolic Enzyme/Protease Autophagy
TargetRenin Autophagy
Specifications
Purity / Grade>98%
SolubilityH2O : ≥ 50 mg/mL (41.00 mM)
Smilessmiles
Misc Information
Alternative NamesCGP 60536;CGP60536B;SPP 100
Observed Molecular Weight1219.59
related data
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