217480-26-7

中文名称 L-803,087 TRIFLUOROACETATE

英文名称 L-803,087 TRIFLUOROACETATE

CAS 217480-26-7

分子式 C25H29F2N5O3

分子量 485.53

MOL 文件 217480-26-7.mol

更新日期 2024/07/18 11:43:10

217480-26-7 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T11800

英文别名

L-803,087 TRIFLUOROACETATE
L-Arginine, N2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-, methyl ester
N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE

物理化学性质

密度1.33±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度Soluble to 100 mM in DMSO and to 100 mM in ethanol

酸度系数(pKa)14.54±0.46(Predicted)

形态Powder

颜色White to light yellow

常见问题列表

生物活性

L-803087 是一种有效的选择性的生长抑素 sst4 受体激动剂，Ki 为 0.7 nM，比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外促进 AMPA 介导的海马突触反应，在体内增加了海藻酸盐诱导的小鼠癫痫发作。

靶点

Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)

体外研究

L-803087 has K _i values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively.
L-803087 has a diamine moiety that maps to lysine on the phmacophore, but relation of this molecule to the aromatic and the Trp substituents of the phmacophore are not obvious. L-803087 does not inhibit secretion of growth hormone, insulin, or glucagon.

体内研究

L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses while facilitation occurred with L-803087 (2 μM).