货号	规格	价格	上海	北京	珠海	武汉
S83923-5mg	99.05%	￥200.00 S83923-5mg ￥200.00 现货	8 8	-	-	-
S83923-10mg	99.05%	￥300.00 S83923-10mg ￥300.00 现货	6 6	-	-	-
S83923-50mg	99.05%	￥820.00 S83923-50mg ￥820.00 现货	6 6	-	-	-
S83923-100mg	≥99%	￥1330.00 S83923-100mg ￥1330.00 2-3天	0 货期：2-3天	-	-	-

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产品描述：

Aliskiren(CGP 60536)是一种renin (肾素)抑制剂，具有降压活性。

靶点：

Renin

体内研究：

In short-term studies, Aliskiren is effective in lowering blood pressure either alone or in combination with valsartan and hydrochlorothiazide, and had a low incidence of serious adverse effects. Aliskiren has a half-life of approximately 40 h, making it suitable for once-daily dosing, with less potential for loss of efficacy between doses than shorter acting agents. Aliskiren exhibits oral bioavailability due to its low molecular weight (609.8 Da) and nonpeptide structure, making it more resistant to gastrointestinal enzyme disintegration. However, it is still poorly absorbed (oral bioavailability, ∼2.5%). Aliskiren is 50% protein bound, and the apparent volume of distribution is 135 L. Aliskiren is slightly metabolized in humans (about 20%) and is approximately 50% metabolized in rodents. Aliskiren effectively reduces functional plasma renin activity by binding to renin with high affinity, preventing it from converting angiotensinogen to angiotensin I. The inhibition of renin by aliskiren is associated with a reduction in circulating levels of angiotensin I and II, with a resultant increase in plasma renin concentration and inhibit activation of mitogen-activated protein kinases ERK1 (p44) and ERK2 (p42). It prevents hypertrophy and proliferation. Aliskiren is well tolerated, with the most common adverse events reported as headache, dizziness, and fatigue

参考文献：

1. Pranay Wal, et al. J Pharm Bioallied Sci. 2011, 3(2): 189–193.

溶解性：

Soluble in DMSO、Ethanol、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.812 ml	9.062 ml	18.123 ml
5 mM	0.362 ml	1.812 ml	3.625 ml
10 mM	0.181 ml	0.906 ml	1.812 ml
50 mM	0.036 ml	0.181 ml	0.362 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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