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CAS No. : 396091-79-5
MCE 国际站:Pasireotide pamoate
产品活性:Pasireotide (SOM230) pamoate 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 pamoate 具有抗分泌、抗增殖和促凋亡活性。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Somatostatin Receptor
In Vitro: Pasireotide pamoate 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 pamoate 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.
In Vivo: Pasireotide pamoate (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 pamoate (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.
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