L-803087

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.

L-803087 has Ki 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).

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GPCR/G Protein

Somatostatin Receptor

Somatostatin

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217480-26-7

485.53

C25H29F2N5O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (514.90 mM; 超声助溶 )

COC(=O)[C@H](CCCNC(N)=N)NC(=O)CCCc1c([nH]c2c(F)cc(F)cc12)-c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years