产品
编 号：F208152
分子式：C64H110N6O16
分子量：1219.59
分子式：C64H110N6O16
分子量：1219.59
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 173334-58-2
产品详情
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.
体内研究：
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.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.
体外研究：
Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro 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.
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.
体内研究：
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.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.
体外研究：
Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro 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.
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