Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate 是一种口服有效的、选择性的肾素 (renin) 抑制剂，IC50为 1.5 nM。Aliskiren hemifumarate 可用于高血压、心血管疾病和癌症恶病质的研究。
| 生物活性 | Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selectiverenininhibitor, withIC50of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases andcancercachexia[1][2][3]. |
| IC50& Target | IC50: 1.5 nM (renin)[1]; 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)[2] |
体外研究
(In Vitro) | Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1].
Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2].
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[2].
Cell Viability Assay[2] | 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. |
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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[3].
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[4].
Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].
| Animal Model: | Sodium-depleted marmosets[3] | | 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[4] | | 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. |
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| 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 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： PBS Solubility: 50 mg/mL (41.00 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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