396091-77-3

396091-77-3结构式

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。

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)

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.