Aliskiren hemifumarate

Modify Date: 2025-08-21 14:06:27

Aliskiren hemifumarate Structure
Aliskiren hemifumarate structure
 Common Name Aliskiren hemifumarate
CAS Number 173334-58-2 Molecular Weight 1219.59000
Density N/A Boiling Point N/A
Molecular Formula C64H110N6O16 Melting Point 72-75?C
MSDS N/A Flash Point N/A

 Use of Aliskiren hemifumarate


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].

 Names

Name Aliskiren hemifumarate
Synonym More Synonyms

 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
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.

 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

δN-Benzyloxycarbonyl Aliskiren structure

δN-Benzyloxycar...

CAS#:1236549-06-6

fumaric acid structure

fumaric acid

CAS#:110-17-8

~97%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: CHEMO IBERICA, S. A.; CARCONE, Luca; MAGRONE, Domenico; BARRECA, Giuseppe; RASPARINI, Marcello; LI MING, Huan Patent: WO2013/14191 A1, 2013 ; Location in patent: Page/Page column 19; 20 ;
tert-butyl N-[(3S,5S,6S,8S)-8-[(3-amino-2,2-dimethyl-3-oxopropyl)carbamoyl]-6-hydroxy-3-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-2,9-dimethyldecan-5-yl]carbamate structure

tert-butyl N-[(...

CAS#:173338-07-3

fumaric acid structure

fumaric acid

CAS#:110-17-8

~86%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: CHEMO IBERICA, S. A.; CARCONE, Luca; MAGRONE, Domenico; BARRECA, Giuseppe; RASPARINI, Marcello; LI MING, Huan Patent: WO2013/14191 A1, 2013 ; Location in patent: Page/Page column 19 ;
fumaric acid structure

fumaric acid

CAS#:110-17-8

Aliskiren structure

Aliskiren

CAS#:173334-57-1

~81%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam Patent: WO2013/61224 A1, 2013 ; Location in patent: Page/Page column 25 ;
Aliskiren Hydrochloride structure

Aliskiren Hydro...

CAS#:173399-03-6

fumaric acid structure

fumaric acid

CAS#:110-17-8

~%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: WO2003/103653 A1, ; Page 196 ; WO 03/103653 A1
fumaric acid structure

fumaric acid

CAS#:110-17-8

BenzeneoctanaMide structure

BenzeneoctanaMide

CAS#:324763-47-5

~%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: WO2012/52829 A1, ; Page/Page column 16-17 ;
3-Amino-2,2-dimethylpropanamide structure

3-Amino-2,2-dim...

CAS#:324763-51-1

~%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: WO2011/148392 A1, ;
3-Methylbutanoic acid structure

3-Methylbutanoi...

CAS#:503-74-2

~%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: WO2011/148392 A1, ;
3-Amino-2,2-dimethylpropanenitrile structure

3-Amino-2,2-dim...

CAS#:67744-70-1

~%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: WO2012/52829 A1, ;
2-cyano-2-methyl-propanamide structure

2-cyano-2-methy...

CAS#:7505-93-3

~%

Aliskiren hemifumarate Structure

Aliskiren hemif...

CAS#:173334-58-2

Literature: WO2011/148392 A1, ;

 Synonyms

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)
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