217480-26-7
217480-26-7 structure
- Name: L-803087
- Chemical Name: L-803,087 trifluoroacetate,N2-[4-(5,7-Difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-L-argininemethylestertrifluoroacetate
- CAS Number: 217480-26-7
- Molecular Formula: C25H29F2N5O3
- Molecular Weight: 599.55000
- Catalog: Signaling Pathways GPCR/G Protein Somatostatin Receptor
- Create Date: 2017-02-20 01:21:23
- Modify Date: 2025-08-24 12:58:57
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L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM, which is > 280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].
| Name | L-803,087 trifluoroacetate,N2-[4-(5,7-Difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-L-argininemethylestertrifluoroacetate |
|---|---|
| Synonyms | l-803,087 trifluoroacetate |
| Description | L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM, which is > 280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2]. |
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| Related Catalog | |
| 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]. |
| References |
| Boiling Point | 779.7ºC at 760mmHg |
|---|---|
| Molecular Formula | C25H29F2N5O3 |
| Molecular Weight | 599.55000 |
| Flash Point | 425.4ºC |
| Exact Mass | 599.21700 |
| PSA | 170.39000 |
| LogP | 5.57200 |
| Vapour Pressure | 1.34E-25mmHg at 25°C |
| Storage condition | -20°C |