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L-803087

Catalog No. T11800 CAS 217480-26-7

L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, which is more than 280-fold more selective than other growth inhibitory receptors.L-803087 induced AMPA-mediated synaptic responses in the hippocampus in vitro, and in vivo increased seizures in alginate-induced seizure-busting mice.

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L-803087, CAS 217480-26-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 198.00
5 mg	In stock	$ 538.00
10 mg	In stock	$ 863.00
25 mg	In stock	$ 1,580.00
50 mg	In stock	$ 2,770.00
100 mg	In stock	$ 4,430.00
1 mL * 10 mM (in DMSO)	In stock	$ 576.00

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Purity: 97.58%

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Description	L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, which is more than 280-fold more selective than other growth inhibitory receptors.L-803087 induced AMPA-mediated synaptic responses in the hippocampus in vitro, and in vivo increased seizures in alginate-induced seizure-busting mice.
Targets&IC50	SST2 receptor:4720 nM (ki), SST1 receptor:199 nM (ki), SST3 receptor:1280 nM (ki), SST5 receptor:3880 nM (ki), SST4 receptor:0.7 nM (ki)
In vitro	L-803087 has Ki values of 199, 4720, 1280, and 3880 nM for cloned human sst1, sst2, sst3, and sst5 receptors, respectively[2]. The molecule L-803087 features a diamine moiety mapping to lysine on the pharmacophore. However, the relationship of this molecule to the aromatic and Trp substituents of the pharmacophore is not apparent. L-803087 does not inhibit the secretion of growth hormone, insulin, or glucagon[2].
In vivo	In wild-type mice, the administration of L-803087 (5 nmol) on average doubles seizure activity. 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, whereas facilitation occurs with L-803087 (2 μM)[1].

Molecular Weight	485.53
Formula	C25H29F2N5O3
CAS No.	217480-26-7

Storage

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

References and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library

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Seglitide acetate CYN 154806 TFA Pasireotide Acetate 2-Aminoethanethiol Cortistatin-14 acetate Cyclosomatostatin Acetate Octreotide Acetate L-796,778 acetate

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Keywords

L-803087 217480-26-7 GPCR/G Protein Somatostatin L 803087 L803087 inhibitor inhibit

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