Pasireotide ditrifluoroacetate||(帕瑞肽二三氟乙酸盐; SOM230 ditrifluoroacetate; Pasireotide TFA salt)-陌孚医药/Medlife

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Pasireotide ditrifluoroacetate (Synonyms: 帕瑞肽二三氟乙酸盐; SOM230 ditrifluoroacetate; Pasireotide TFA salt)

目录号: PL11412 纯度: ≥99%

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PL11412-10mM*1mLinDMSO	10mM*1mLinDMSO	¥24801.00	请登录

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中文名称	Pasireotide ditrifluoroacetate
英文名称	Pasireotide ditrifluoroacetate
包装储存	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Pasireotide (SOM230) ditrifluoroacetate 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 ditrifluoroacetate 具有抗分泌、抗增殖和促凋亡活性。

生物活性

Pasireotide (SOM230) ditrifluoroacetate, 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 ditrifluoroacetate 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 ditrifluoroacetate 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 ditrifluoroacetate 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 ditrifluoroacetate (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 ditrifluoroacetate (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

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 : 100 mg/mL (78.42 mM; Need ultrasonic)H₂O : 33.33 mg/mL (26.14 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

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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