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: 2024-01-07 21:19:40
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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor Research Areas >> Neurological Disease
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	[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.

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

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