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中文名称N/A
中文同义词化合物 Pasireotide pamoate
英文名称Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl], 4,4'-methylenebis[3-hydroxy-2-naphthalenecarboxylate] (1:1)
英文同义词Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl], 4,4'-methylenebis[3-hydroxy-2-naphthalenecarboxylate] (1:1);SOM230 pamoate;Pasireotide PamoateQ: What is Pasireotide Pamoate Q: What is the CAS Number of Pasireotide Pamoate Q: What is the storage condition of Pasireotide Pamoate;Pasireotide pamoate
CAS号396091-79-5
分子式C58 H66 N10 O9 . C23 H16 O6
分子量1435.6
EINECS号
相关类别
Mol文件396091-79-5.mol
结构式N/A 结构式

N/A 性质

N/A 用途与合成方法

Pasireotide pamoate (SOM230 pamoate) 是一种稳定的环己肽生长激素抑制素(somatostatin)类似物,对具有人 somatostatin 受体具有拮抗作用,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 。

pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)

Pasireotide pamoate exhibits unique high-affinity binding to human somatostatin receptors.
Pasireotide pamoate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells with an IC 50 of 0.4±0.1 nM.

Pasireotide pamoate (160mg/Kg/month; s.c.; for 4 months) decreases serum insulin levels and increases serum glucose levels in Pdx1-Cre.
Pasireotide pamoate displays a reduction in tumor activity and reduces Pancreatic Neuroendocrine Tumor (PNET) size in Pdx1-Cre.
Pasireotide pamoate increases apoptosis in PNETs in Pdx1-Cre.
Pasireotide pamoate exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in in a mouse model of immune-mediated arthritis.

Animal Model: Eight 12-month old mice carrying the Men1 allele, Men1 floxed/floxed conditional knockout (Pdx1-Cre)
Dosage: 60mg/kg
Administration: Subcutaneous injection; very month; for 4 months
Result: Decreased serum insulin levels and increases serum glucose levels in Pdx1-Cre.

安全信息

MSDS信息

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"N/A"相关产品信息
帕西瑞肽 醋酸兰瑞肽 C[AMINOHEPTANOYL-PHE-DTRP-LYS-THR:BZL] DOTA-NOC 醋酸奥曲肽
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