Pasireotide

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Pasireotide

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

396091-73-9

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

帕瑞肽
SOM230

产品介绍

Pasireotide (SOM230) 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 可以抑制 GH、IGF-I 和 ACTH 的分泌，可用于研究肢端肥大症和库欣病。Pasireotide 还具有抗分泌、抗增殖和促凋亡活性。

生物活性

Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity atsomatostatin receptors(subtypessst1/2/3/4/5,pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity^[1]^[2]^[3].

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 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)^[1].
Pasireotide effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC₅₀of 0.4 nM^[1].

体内研究
(In Vivo)

Pasireotide (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis inPdx1-Cre^[2].
Pasireotide (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^[4].

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

1047.21

Formula

C₅₈H₆₆N₁₀O₉

CAS 号

396091-73-9

Sequence

Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-Lys-{Tyr(4-Bzl)}-Phe]

Sequence Shortening

Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-K-{Tyr(4-Bzl)}-F]

中文名称

帕瑞肽；帕西瑞肽

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.