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Aliskiren Hemifumarate — Datasheet

CAT. NO. DCAPI1495

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ParameterValue
Chemical NameAliskiren hemifumarate
CAS No.173334-58-2
SynonymsAliskiren hemifumarate;(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide hemifumarate;ALISKIREN FUMARATE;(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide hemifumarate;CGP 60536;CGP60536B;Rasilez;SPP 100;Tekturna;(2S,4S,5S,7S)-N-(2-Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate;CGP-60536;SPP-100;Unii-C8A0p8G029;skiren heMifuMarate;Rasilez HeMifuMarate;Tekturna HeMifuMarate;Aliskiren-D6 HeMifuMarate;(αS,γS,δS,zS)-δ-AMino-N-(3-aMino-2,2-diMethyl-3-oxopropyl)-γ-hydroxy-4-Methoxy-3-(3-Methoxypropoxy)-α,z-bis(1-Methylethyl)benzeneoctanaMide HeMifuMarate;(2S,4S,5S,7S)-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-8-methylnonanamide hemifumarate
Formula2(C30H53N3O6).C4H4O4
M.Wt1219.6
SMILESO=C(O)/C=C/C(O)=O.O=C(NCC(C)(C(N)=O)C)[C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)CC1=CC=C(OC)C(OCCCOC)=C1)N)O)C(C)C.O=C(NCC(C)(C(N)=O)C)[C@H](C(C)C)C[C@H](O)[C@@H](N)C[C@@H](C(C)C)CC2=CC=C(OC)C(OCCCOC)=C2
Purity>99%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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