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

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].

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].

1786412-46-1

C27H30F5N5O5

599.559

L-803087 TFA

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years