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L-803087 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-803087 TFA图片
CAS NO:1786412-46-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
L-803087 TFA 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,对sst4的选择性比其他生长抑素受体高 280 倍以上。L-803087 TFA 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。
生物活性

L-803087 TFA is a potent and selectivesomatostatin sst4 receptoragonist with aKiof 0.7 nM. L-803087 TFA is >280-fold more selective forsst4 receptorthan other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].

IC50& Target

Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)[1]

体外研究
(In Vitro)

L-803087 hasKivalues for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively[1].
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[1].

体内研究
(In Vivo)

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)[2].

分子量

599.55

Formula

C27H30F5N5O5

CAS 号

1786412-46-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.