L-803,087 TRIFLUOROACETATE
| 中文名称 | L-803,087 TRIFLUOROACETATE |
|---|---|
| 中文同义词 | 化合物 T11800 |
| 英文名称 | L-803,087 TRIFLUOROACETATE |
| 英文同义词 | N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE;L-803,087 TRIFLUOROACETATE;L-Arginine, N2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-, methyl ester;L803087,L 803087 |
| CAS号 | 217480-26-7 |
| 分子式 | C25H29F2N5O3 |
| 分子量 | 485.53 |
| EINECS号 | |
| 相关类别 | Somatostatin receptor |
| Mol文件 | 217480-26-7.mol |
| 结构式 |  |
L-803,087 TRIFLUOROACETATE 性质
| 密度 | 1.33±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 在 DMSO 中溶解度为 100 mM，在乙醇中溶解度为 100 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 14.54±0.46(Predicted) |
| 颜色 | 白色至浅黄色 |
Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)
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.
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).