Aliskiren

Modify Date: 2024-01-02 18:31:54

Aliskiren structure	Common Name	Aliskiren
	CAS Number	173334-57-1	Molecular Weight	551.758
	Density	1.1±0.1 g/cm3	Boiling Point	748.4±60.0 °C at 760 mmHg
	Molecular Formula	C₃₀H₅₃N₃O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	406.4±32.9 °C

Use of Aliskiren

Aliskiren(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].

Name	aliskiren
Synonym	More Synonyms

Description	Aliskiren(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. [5]. Chang AY, et al. Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. Neurobiol Dis. 2014 Nov;71:292-304.

Description

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.

[5]. Chang AY, et al. Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. Neurobiol Dis. 2014 Nov;71:292-304.

Density	1.1±0.1 g/cm3
Boiling Point	748.4±60.0 °C at 760 mmHg
Molecular Formula	C₃₀H₅₃N₃O₆
Molecular Weight	551.758
Flash Point	406.4±32.9 °C
Exact Mass	551.393433
PSA	146.13000
LogP	2.74
Vapour Pressure	0.0±2.6 mmHg at 25°C
Index of Refraction	1.514

Hazard Codes	Xi

Precursor 8
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CAS#:173334-58-2 Aliskiren hemif... CAS#:172900-70-8 (R)-2-[3-(3-MET... CAS#:172900-71-9 (R)-2-[3-(3-MET... CAS#:324763-39-5 4-[(2R)-2-(Chlo...
DownStream 1
CAS#:173334-58-2 Aliskiren hemif...