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编 号：F208225
分子式：C30H54ClN3O6
分子量：588.22
分子式：C30H54ClN3O6
分子量：588.22
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CAS No: 173399-03-6
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生物活性：
Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia-.
体内研究：
Aliskiren hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively.Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration.Aliskiren hydrochloride (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) hydrochloride is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia-.
体内研究：
Aliskiren hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively.Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration.Aliskiren hydrochloride (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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