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L-803087 TFA

Catalog No. T39207 CAS 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.

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L-803087 TFA, CAS 1786412-46-1

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	SST2 receptor:4720 nM (Ki), SST4 receptor:0.7 nM (Ki), SST1 receptor:199 nM (Ki), SST3 receptor:1280 nM (Ki), SST5 receptor:3880 nM (Ki)
In vitro	L-803087 exhibits affinity for cloned human sst1, sst2, sst3, and sst5 receptors with K_i values of 199, 4720, 1280, and 3880 nM, respectively[1]. It features a diamine moiety aligned with lysine on the pharmacophore; however, the connection between this molecule and the pharmacophore's aromatic and Trp (tryptophan) substituents remains unclear. Additionally, L-803087 does not suppress the secretion of growth hormone, insulin, or glucagon[1].
In vivo	Administering 5 nmol of L-803087 on average doubles seizure activity in wild-type mice, an effect that is inhibited by 3 nmol of Octreotide. Additionally, in hippocampal slices from wild-type mice, 2 μM Octreotide does not alter AMPA-mediated synaptic responses, whereas 2 μM L-803087 induces facilitation[2].

Molecular Weight	599.559
Formula	C27H30F5N5O5
CAS No.	1786412-46-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Rohrer SP, et al. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40. 2. Moneta D, et al. Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur J Neurosci. 2002 Sep;16(5):843-9.

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Keywords

L-803087 TFA 1786412-46-1 L803087 TFA L 803087 TFA inhibitor inhibit

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