Pasireotide L-aspartate salt (Synonyms: 帕瑞肽天门冬氨酸盐; SOM230 L-aspartate)
目录号: PL11407 纯度: ≥98.0%
CAS No. :396091-77-3
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中文名称
Pasireotide L-aspartate salt
英文名称
Pasireotide L-aspartate salt
英文别名
Pasireotide (L-aspartate salt);SOM230 L-aspartate;Pasireotide L-aspartate salt
Cas No.
396091-77-3
分子式
C62H73N11O13
分子量
1180.31
包装储存
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
产品详情
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。
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.
性状
Solid
IC50 & Target[1][2]
pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)
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).
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. 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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 1 mg/mL (0.85 mM; Need ultrasonic)
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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