L-803087

• CAT Number: I010485
• CAS Number: 217480-26-7
• Molecular Formula: C25H29F2N5O3
• Molecular Weight: 485.53
• Purity: ≥95%
• Synonyms: methyl (2S)-5-(diaminomethylideneamino)-2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)butanoylamino]pentanoate
• InChI: InChI=1S/C25H29F2N5O3/c1-35-24(34)20(10-6-12-30-25(28)29)31-21(33)11-5-9-17-18-13-16(26)14-19(27)23(18)32-22(17)15-7-3-2-4-8-15/h2-4,7-8,13-14,20,32H,5-6,9-12H2,1H3,(H,31,33)(H4,28,29,30)/t20-/m0/s1
• InChIKey: OPNMQSFIGUSHDH-FQEVSTJZSA-N
• SMILES: COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C1C=C(C=C2F)F)C3=CC=CC=C3

L-803087(CAT: I010485) is a potent and highly selective somatostatin sst₄ receptor agonist with a Ki of 0.7 nM, showing over 280-fold selectivity against other somatostatin receptor subtypes. Binding assays demonstrate weak activity at sst₁, sst₂, sst₃, and sst₅ receptors (Ki values of 199, 4720, 1280, and 3880 nM, respectively). Functionally, L-803087 facilitates AMPA-mediated hippocampal synaptic responses and significantly enhances kainate-induced seizure activity in vivo, effects blocked by the somatostatin analog Octreotide. Unlike other somatostatin ligands, it does not inhibit growth hormone, insulin, or glucagon secretion. L-803087 is a valuable probe for investigating sst₄ receptor function, neural excitability, and synaptic modulation.