1. GPCR/G Protein
    Neuronal Signaling
  2. Somatostatin Receptor
  3. L-803087 TFA

L-803087 TFA 

Cat. No.: HY-108497A
Handling Instructions

L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki 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.

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L-803087 TFA Chemical Structure

L-803087 TFA Chemical Structure

CAS No. : 1786412-46-1

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Description

L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki 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[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]

In Vitro

L-803087 has Ki 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].

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].

Molecular Weight

599.55

Formula

C₂₇H₃₀F₅N₅O₅

CAS No.

1786412-46-1

SMILES

FC(F)(C(O)=O)F.N=C(N)NCCC[[email protected]@H](C(OC)=O)NC(CCCC1=C(C2=CC=CC=C2)NC3=C1C=C(F)C=C3F)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

L-803087L803087L 803087Somatostatin ReceptorSSTRsSSTRsst4seizureshippocampalsynapticAMPAdiamineInhibitorinhibitorinhibit

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L-803087 TFA
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HY-108497A
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