Aliskiren hemifumarate(Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate)

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Aliskiren hemifumarate (Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate) 纯度: 98.98%

Aliskiren hemifumarate (CGP 60536 hemifumarate) 是肾素的直接抑制剂，IC50为1.5 nM。

Aliskiren hemifumarate(Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate)

Aliskiren hemifumarate Chemical Structure

CAS No. : 173334-58-2

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10 mM * 1 mL in Water ￥698 In-stock
10 mg ￥520 In-stock
50 mg ￥1100 In-stock
100 mg ￥1800 In-stock
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生物活性

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].

Clinical Trial

分子量

1219.59

Formula

C64H110N6O16
CAS 号

173334-58-2
中文名称

阿利克仑半富马酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : ≥ 50 mg/mL (41.00 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8199 mL 4.0997 mL 8.1995 mL
5 mM 0.1640 mL 0.8199 mL 1.6399 mL
10 mM 0.0820 mL 0.4100 mL 0.8199 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

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