Pasireotide L-aspartate salt - CAS:396091-77-3

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

目录号 : KM17928 CAS No. : 396091-77-3 纯度 : 98%

Data Sheet 产品使用指南

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。

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1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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, 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.

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.

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.

分子式

C₆₂H₇₃N₁₁O₁₃

分子量

1180.31

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

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

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

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