L-803,087 TRIFLUOROACETATE
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 |
L-803,087 TRIFLUOROACETATE 用途与合成方法
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).
