SKU : MC531543
CAS Number : 173334-58-2
Molecular Formula : C64H110N6O16 | Molecular Weight : 1219.59
Synonyms : CGP 60536 (hemifumarate);CGP60536B (hemifumarate);SPP 100 (hemifumarate)
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | Aliskiren (hemifumarate) |
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CAS Number | 173334-58-2 |
MDL Number | MFCD10566724 |
Molecular Formula | C64H110N6O16 |
Molecular Weight | 1219.59 |
Synonyms | CGP 60536 (hemifumarate);CGP60536B (hemifumarate);SPP 100 (hemifumarate) |
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].
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