L-803087 TFA

Name: L-803087 TFA
Brand: TargetMol
SKU: T39207
Rating: 4.5 (1 reviews)

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产品编号 T39207Cas号 1786412-46-1

L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.

L-803087 TFA

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产品编号 T39207Cas号 1786412-46-1

规格	价格	库存	数量
100 mg	询价	期货
500 mg	询价	期货

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产品描述	L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.
靶点活性	SST5 receptor:3880 nM (Ki), SST3 receptor:1280 nM (Ki), SST1 receptor:199 nM (Ki), SST4 receptor:0.7 nM (Ki), SST2 receptor:4720 nM (Ki)
体外活性	L-803087 has K i values 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].
体内活性	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].