396091-77-3

• 常用中文名：Pasireotide L-天冬氨酸盐
• 常用英文名：Pasireotide L-aspartate salt
• CAS号：396091-77-3
• 分子式：C₆₂H₇₃N₁₁O₁₃
• 分子量：1180.309
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 生长抑素受体
• 发布时间：2018-05-26 00:05:43
• 更新时间：2024-01-06 17:50:03
• Pasireotide(SOM 230)是一环六肽类somatostatin模拟类似物,对人somatostatin受体有很高的亲和力,对SST1、2、3、4和5的pKi值分别为8.2、9.0、9.1、<7.0和9.9。

名称

• 中文名: Pasireotide L-天冬氨酸盐
• 英文名: Pasireotide L-aspartate salt
• 英文别名: L-Aspartic acid, compd. with cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl] (1:1); Pasireotide L-aspartate salt; L-Aspartic acid - cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-benzyl-L-tyrosyl-L-phenylalanyl-(4R)-4-{[(2-aminoethyl)carbamoyl]oxy}-L-prolyl] (1:1); Pasireotide (L-aspartate salt)

物化性质

• 分子式: C₆₂H₇₃N₁₁O₁₃
• 分子量: 1180.309
• 精确质量: 1179.538940
• 储存条件: 2-8℃

生物活性

• 描述: Pasireotide(SOM 230)是一环六肽类somatostatin模拟类似物,对人somatostatin受体有很高的亲和力,对SST1、2、3、4和5的pKi值分别为8.2、9.0、9.1、<7.0和9.9。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 生长抑素受体
  研究领域 >> 内分泌
• 参考文献:

  [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]. Hofland LJ, et al. The novel somatostatin analog SOM230 is a potent inhibitor of hormone release by growth hormone- and prolactin-secreting pituitary adenomas in vitro. J Clin Endocrinol Metab. 2004 Apr;89(4):1577-85.

  [3]. Murray RD, et al. The novel somatostatin ligand (SOM230) regulates human and rat anterior pituitary hormone secretion. J Clin Endocrinol Metab. 2004 Jun;89(6):3027-32.

  [4]. 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.

  [5]. 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.