Aliskiren Hemifumarate

A nonpeptide renin inhibitor

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100mg

￥1737.00

1390.00

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1g

￥2737.00

2190.00

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货号: ajci10688
CAS: 173334-58-2
别名: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate
分子式: C64H110N6O16
分子量: 1219.59
纯度: >98%
溶解度: ≥ 58.5mg/mL in DMSO, ≥ 121.9mg/mL in EtOH with gentle warming, ≥ 122mg/mL in Water with gentle warming
储存: Store at -20°C
库存: 现货

Background

Aliskiren hemifumarate(CGP 60536 hemifumarate) 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].

参考文献:
[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.