Pasireotide L-aspartate salt(Synonyms: 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Pasireotide L-aspartate salt (Synonyms: 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate) 纯度: 99.44%

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 pKi 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。

Pasireotide L-aspartate salt(Synonyms: 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate)

Pasireotide L-aspartate salt Chemical Structure

CAS No. : 396091-77-3

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1 mg ￥2100 In-stock
5 mg ￥6900 In-stock
10 mg ￥11000 In-stock
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Pasireotide L-aspartate salt 相关产品

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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, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2].

IC50 & Target

pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]
体外研究
(In Vitro)

Pasireotide L-aspartate salt exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively)[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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[2].
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[3].

上海金畔生物科技有限公司 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[2]
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.

Clinical Trial

分子量

1180.31

Formula

C62H73N11O13
CAS 号

396091-77-3
中文名称

帕瑞肽天门冬氨酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 1 mg/mL (0.85 mM; Need ultrasonic)
参考文献

  • [1]. Lewis I, et, al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem. 2003 Jun 5;46(12):2334-44.

    [2]. Quinn TJ, et, al. Pasireotide (SOM230) is effective for the treatment of pancreatic neuroendocrine tumors (PNETs) in a multiple endocrine neoplasia type 1 (MEN1) conditional knockout mouse model. Surgery. 2012 Dec;152(6):1068-77.

    [3]. Imhof AK, et, al. Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62.

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