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编 号:F346770
分子式:C60H70N10O11
分子量:1107.26
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1mg
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5mg
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10mg
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生物活性:
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.

体内研究:
Pasireotide acetate (160 mg/kg/月;皮下注射 4 个月) 显著降低血清胰岛素,增加血清葡萄糖,减小肿瘤大小并增加 Pdx1-Cre 细胞凋亡。 Pasireotide acetate (2-50 μg/kg;皮下注射,每天两次,持续 42 天) 在免疫介导的关节炎小鼠模型中通过 SSTR2 受体发挥镇痛和抗炎作用。Animal Model:12 month-old conditional Men1 knockout mice with insulinoma
Dosage:160 mg/kg/mouth
Administration:S.c. every month for 4 months
Result:Decreased the serum insulin from 1.060 μg/L to 0.3653 μg/L and increased the serum glucose from 4.246 mM to 7.122 mM.Significantly reduced the tumor size and increased apoptosis.

体外研究:
Pasireotide acetate与人生长抑素受体 (亚型 sst1/2/3/4/5,pKi=8.2/9.0/9.1/Pasireotide acetate 相关抗体:
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