Aliskiren Hemifumarate|173334-58-2|(阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate)-陌孚医药/Medlife

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

目录号: PC14959 纯度: ≥98%

CAS No. :173334-58-2

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中文名称	Aliskiren Hemifumarate
中文别名	阿利克仑半富马酸盐;(2S,4S,5S,7S)-5-氨基-N-(2-氨基甲酰基-2-甲基丙基)-4-羟基-2-异丙基-7-[4-甲氧基-3-(3-甲氧基丙氧基)苄基]-8-甲基壬酰胺半富马酸盐;阿立克仑半富马酸盐;阿利吉仑;阿利吉仑-D6半富马酸盐;阿利吉仑半富马酸盐标准品;阿利克伦富马酸盐;富马酸阿利吉仑;还阳碱;阿利克伦半富马酸;半延胡索酸阿利吉仑;阿利G仑半富马酸盐;阿利克伦扮富马酸盐;阿里克伦半富马酸盐;阿利吉仑半富马酸盐;阿利吉仑ALISKIRENHEMIFUMARATE(研发中)
英文名称	Aliskiren Hemifumarate
英文别名	Aliskiren hemifumarate;(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide hemifumarate;ALISKIREN FUMARATE;(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide hemifumarate;CGP 60536;CGP60536B;Rasilez;SPP 100;Tekturna;(2S,4S,5S,7S)-N-(2-Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate;CGP-60536;SPP-100;Unii-C8A0p8G029;skiren heMifuMarate;Rasilez HeMifuMarate;Tekturna HeMifuMarate;Aliskiren-D6 HeMifuMarate;(αS,γS,δS,zS)-δ-AMino-N-(3-aMino-2,2-diMethyl-3-oxopropyl)-γ-hydroxy-4-Methoxy-3-(3-Methoxypropoxy)-α,z-bis(1-Methylethyl)benzeneoctanaMide HeMifuMarate;(2S,4S,5S,7S)-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-8-methylnonanamide hemifumarate
Cas No.	173334-58-2
分子式	₂(C₃₀H₅₃N₃O₆)^.C₄H₄O₄
分子量	1219.60
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC₅₀ of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.

性状

Solid

IC50 & Target[1][2]

IC50: 1.5 nM (renin); 0.6 nM (human renin), 2 nM (marmoset renin), 80 nM (rat renin), 7 nM (dog renin), 11 nM (rabbit renin), 63 nM (guinea pig renin), 150 nM (pig renin)

体外研究(In Vitro)

Aliskiren hemifumarate inhibits plasma renin activity (PRA) 体外研究 with IC₅₀s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively.
Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration.
Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Smooth muscle cell (SMC)
Concentration:	1-10 μM
Incubation Time:	24 hours
Result:	Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.

体内研究(In Vivo)

Aliskiren hemifumarate (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets.
Aliskiren hemifumarate (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole?body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting.
Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Sodium-depleted marmosets
Dosage:	3 mg/kg, 10 mg/kg
Administration:	Oral gavage; once daily; 12 days
Result:	Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate. Showed no rebound increase in BP following the end of treatment with either dose of aliskiren. Inhibited the RAS and controls the upregulation of pro?inflammatory cytokines.

Animal Model:	Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells
Dosage:	10 mg/kg
Administration:	Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection
Result:	Enhanced grip strength, coordination, and locomotor activity. Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor?α (TNF?α) and inter? leukin?6 (IL?6) levels.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

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]. Ferri N, et al. Aliskiren inhibits prorenin-induced human aortic smooth muscle cell migration. J Renin Angiotensin Aldosterone Syst. 2015 Jun;16(2):284-91. [Information]

[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. [Information]

[4]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022. [Information]

[5]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31. [Information]

[6]. 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. [Information]

溶解度数据

体外研究:

H₂O : ≥ 50 mg/mL (41.00 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (41.00 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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