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Aliskiren

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Chemical Structure| 173334-57-1 同义名 : SPP 100;CGP 60536;Aliskiren, Enviage, Rasilez, Riprazo, SPP100, Sprimeo;CGP60536B
CAS号 : 173334-57-1
货号 : A227203
分子式 : C30H53N3O6
纯度 : 99%+
分子量 : 551.758
MDL号 : MFCD09839018
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(190.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(181.24 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
靶点

  • Renin

    Renin, IC50:1.5 nM
描述 Aliskiren is an orally active renin inhibitor with IC50 value of 0.6nM, used as antihypertensive drugs that block the first step in the renin–angiotensin system, which can interrupt the negative feedback effects of angiotensin II on renin secretion. Administration of Aliskiren at dose of 150mg alone significantly inhibited plasma renin activity by 65% in patients with hypertension. Inhibition of renin by Aliskiren in combinations with hydrochlorothiazide, ramipril, or irbesartan increased renin–angiotensin system suppression, improved 24-hour blood pressure control.
作用机制 Aliskiren interacts with several binding pockets in distinct regions around the active site of renin.[2]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00865020 - Completed - -
NCT00841672 Moderate to Severe Hypertensio... 展开 >>n 收起 << Phase 3 Completed - Germany ... 展开 >> Investigative Site Berlin, Germany Philippines Investigative Site Manilla, Philippines Romania Investigative Site Bucharest, Romania Russian Federation Investigative Site Moscow, Russian Federation Singapore Investigative Site Singapore, Singapore Spain Investigative Site Madrid, Spain 收起 <<
NCT00841672 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.06mL

1.81mL

0.91mL

18.12mL

3.62mL

1.81mL
参考文献

[1]Wal P, Wal A, et al. Aliskiren: An orally active renin inhibitor. J Pharm Bioallied Sci. 2011 Apr;3(2):189-93.

[2]Jensen C, Herold P, et al. Aliskiren: the first renin inhibitor for clinical treatment. Nat Rev Drug Discov. 2008 May;7(5):399-410.

[3]O'Brien E, Barton J, et al. Aliskiren reduces blood pressure and suppresses plasma renin activity in combination with a thiazide diuretic, an angiotensin-converting enzyme inhibitor, or an angiotensin receptor blocker. Hypertension. 2007 Feb;49(2):276-84. Epub 2006 Dec 11.

[4]Feldman DL, Jin L, et al. Effects of aliskiren on blood pressure, albuminuria, and (pro)renin receptor expression in diabetic TG(mRen-2)27 rats. Hypertension. 2008 Jul;52(1):130-6.

[5]Wood JM, Schnell CR, et al. Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats. J Hypertens. 2005 Feb;23(2):417-26.

[6]Un H, Bayir Y, et al. The Effects of RAAS Inhibition in Rate Limiting Step by Aliskiren on Testicular Torsion Injury in Rats. J Urol. 2015 Sep;194(3):828-33.

[7]Higashikuni Y, Takaoka M, et al. Aliskiren in combination with valsartan exerts synergistic protective effects against ventricular remodeling after myocardial infarction in mice. Hypertens Res. 2012 Jan;35(1):62-9.

[8]Dong YF, Liu L, et al. Aliskiren prevents cardiovascular complications and pancreatic injury in a mouse model of obesity and type 2 diabetes. Diabetologia. 2010 Jan;53(1):180-91.

[9]Aliskiren