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编 号：F744322
分子式：C49H66N10O10S2.xC23H16O6
分子式：C49H66N10O10S2.xC23H16O6
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CAS No: 135467-16-2
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生物活性：
Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
体内研究：
Octreotide pamoate (subcutaneous injection, 30 mg/kg, once) can inhibit tumor growth significantly with no effect on body weight.Octreotide pamoate (intramuscular injection, 60 mg/kg, every 21 days, 42 days) inhibits serum insulin-like growth factor (IGF-I) without toxicity in dogs with appendicular osteosarcoma (OSA).Octreotide pamoate (subcutaneous injection, 40 μg/kg, Every 12 hours, 8 days) improves hepatic glycogen synthesis in obese male Sprague?Dawley (SD) rats.Animal Model:Female nude mice (nu/nu Balbc-A weighing 19-22 g)
Dosage:30 mg/kg
Administration:Subcutaneous injection; once
Result:Showed that the average volume of tumors treated was 25.8% of the control group and no effect on body weight.
Animal Model:Dogs with appendicular OSA
Dosage:60 mg/kg
Administration:Intramuscular injection; every 21 days; 42 days
Result:Resulted in a 43% decrease in mean serum IGF-I compared with mean baseline concentrations.
Animal Model:Male Sprague?Dawley (SD) rats (3 weeks; 40-60 g)
Dosage:40 μg/kg
Administration:Subcutaneous injection; every 12 hours; 8 days
Result:Significantly improved fat deposition and reduced lipid infiltration.
体外研究：
Octreotide pamoate (10?8mM, 6 hours) induces phosphorylated?glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity.
Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
体内研究：
Octreotide pamoate (subcutaneous injection, 30 mg/kg, once) can inhibit tumor growth significantly with no effect on body weight.Octreotide pamoate (intramuscular injection, 60 mg/kg, every 21 days, 42 days) inhibits serum insulin-like growth factor (IGF-I) without toxicity in dogs with appendicular osteosarcoma (OSA).Octreotide pamoate (subcutaneous injection, 40 μg/kg, Every 12 hours, 8 days) improves hepatic glycogen synthesis in obese male Sprague?Dawley (SD) rats.Animal Model:Female nude mice (nu/nu Balbc-A weighing 19-22 g)
Dosage:30 mg/kg
Administration:Subcutaneous injection; once
Result:Showed that the average volume of tumors treated was 25.8% of the control group and no effect on body weight.
Animal Model:Dogs with appendicular OSA
Dosage:60 mg/kg
Administration:Intramuscular injection; every 21 days; 42 days
Result:Resulted in a 43% decrease in mean serum IGF-I compared with mean baseline concentrations.
Animal Model:Male Sprague?Dawley (SD) rats (3 weeks; 40-60 g)
Dosage:40 μg/kg
Administration:Subcutaneous injection; every 12 hours; 8 days
Result:Significantly improved fat deposition and reduced lipid infiltration.
体外研究：
Octreotide pamoate (10?8mM, 6 hours) induces phosphorylated?glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity.
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