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Aliskiren hemifumarate

Names

[ CAS No. ]:
173334-58-2

[ Name ]:
Aliskiren hemifumarate

[Synonym ]:
CGP60536B
Aliskiren fumarate
tekturna
(2S,4S,5S,7S)-5-Amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide (2E)-2-butenedioate (2:1)
Aliskiren hemifumarate
(2E)-But-2-endisäure--(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methyl-2-(1-methylethyl)nonanamid(1:2)
Benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS,γS,δS,ζS)-, (2E)-2-butenedioate (2:1) (salt)
CGP 60536
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methyl-2-(1-methylethyl)nonanamide (2E)-but-2-enedioate (2:1) (salt)
Benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS,γS,δS,ζS)-, (2E)-2-butenedioate (2:1&#xD; ) (salt)
acide (2E)-but-2-ènedioïque - (2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-diméthyl-3-oxopropyl)-4-hydroxy-7-[4-méthoxy-3-(3-méthoxypropoxy)benzyl]-8-méthyl-2-(1-méthyléthyl)nonanamide (1:2)
Rasilez
SPP 100
(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
benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS,γS,δS,ζS)-, (2E)-2-butenedioate (2:1
Aliskirenhemifumarate
Aliskiren (hemifumarate)

Biological Activity

[Description]:

Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.IC50 value: 1.5 nM [1]Target: reninin 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].

[Related Catalog]:

Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Metabolic Enzyme/Protease >> Renin
Research Areas >> Cardiovascular Disease

[References]

[1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758

[2]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31.

[3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705.

[4]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018.


[Related Small Molecules]

VTP 27999 trifluoroacetate | ACT 178882 | Handle region peptide, rat

Chemical & Physical Properties

[ Melting Point ]:
72-75?C

[ Molecular Formula ]:
C64H110N6O16

[ Molecular Weight ]:
1219.59000

[ Exact Mass ]:
1218.80000

[ PSA ]:
366.86000

[ LogP ]:
9.88180

[ Vapour Pressure ]:
1.59E-23mmHg at 25°C

[ Storage condition ]:
Hygroscopic, -20°C Freezer, Under Inert Atmosphere

Safety Information

[ Hazard Codes ]:
Xi

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds