| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H30F5N5O5 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
L-803087 TFA is a potent, selective sst4 somatostatin receptor agonist with a Ki of 0.7 nM, showing more than 280-fold selectivity for sst4 over other somatostatin receptor subtypes. It enhances AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].
It has the molecular formula C27H30F5N5O5 and a molecular weight of 599.55 g/mol.
Physical & Chemical Properties
| CAS Number | 1786412-46-1 |
|---|---|
| Molecular Formula | C27H30F5N5O5 |
| Molecular Weight | 599.55 g/mol |
| SMILES | FC(F)(C(O)=O)F.N=C(N)NCCC[C@@H](C(OC)=O)NC(CCCC1=C(C2=CC=CC=C2)NC3=C1C=C(F)C=C3F)=O |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & 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]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
For cloned human sst1, sst2, sst3 and sst5 receptors, L-803087 has Ki values of 199, 4720, 1280 and 3880 nM, respectively[1]. The diamine moiety of L-803087 maps to lysine on the pharmacophore, but how this molecule relates to the aromatic and Trp substituents of the pharmacophore is not obvious. Secretion of growth hormone, insulin, or glucagon is not inhibited by L-803087[1].
In Vivo
In wild-type mice, L-803087 (5 nmol) doubles seizure activity on average. Interestingly, 3 nmol Octreotide blocks this effect. In hippocampal slices from wild-type mice, Octreotide (2 μM) leaves AMPA-mediated synaptic responses unchanged, whereas facilitation occurs with L-803087 (2 μM)[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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