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


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 sst1/2/3/4/5pKi 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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Pasireotide L-aspartate salt 相关产品


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  • Macrocyclic Compound Library


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]

(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.

(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










Room temperature in continental US; may vary elsewhere.


4°C, sealed storage, away from moisture

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

In Vitro: 

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

  • [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.