Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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L-803087 217480-26-7 GPCR/G Protein Somatostatin L 803087 L803087 inhibitor inhibit