Pasireotide L-aspartate salt 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate|cas:396091-77-3|西域试剂

Pasireotide L-aspartate salt 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate,98.0%

产品编号：Bellancom-79136| CAS NO：396091-77-3| 分子式：C₆₂H₇₃N₁₁O₁₃| 分子量：1180.31

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货号	价格	库存与货期
Bellancom-79136	￥2100.00	杭州北京（现货）
Bellancom-79136	￥6900.00	杭州北京（现货）
Bellancom-79136	￥11000.00	杭州北京（现货）

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Pasireotide L-aspartate salt 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate

产品介绍

Pasireotide (SOM230) L-aspartate salt 是一种长效的环己肽生长激素抑制素类似物，可以提高生长抑素受体的激动剂活性，对 sst1/2/3/4/5 的 pK_i 分别为 8.2/9.0/9.1/<7.0/9.9。Pasireotide L-aspartate salt 具有抗分泌、抗增殖和促凋亡活性。

生物活性

Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.

体外研究

Pasireotide L-aspartate salt exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively).
Pasireotide L-aspartate salt effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC₅₀ of 0.4 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Pasireotide L-aspartate salt (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre.
Pasireotide L-aspartate salt (2-50 μg/kg; s.c. twice daily for 42 days) exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.