L-803087

SKU: orb1709296

Description

L-803087 is a highly selective sst4 receptor agonist (Ki = 0.7 nM) with over 280-fold selectivity. It potentiates AMPA-mediated synaptic responses in hippocampal studies in vitro and has been shown to exacerbate seizures in alginate-induced seizure models in vivo, supporting its use in neuroscience research.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 217480-26-7
• MW: 485.53
• Purity: 99.37% (May vary between batches)
• Formula: C₂₅H₂₉F₂N₅O₃
• SMILES: COC(=O)[C@H](CCCNC(N)=N)NC(=O)CCCc1c([nH]c2c(F)cc(F)cc12)-c1ccccc1
• Target: Somatostatin
• Solubility: DMSO:55 mg/mL (113.28 mM)

Bioactivity

• Target IC50:
  SST3 receptor:1280 nM (ki)|SST4 receptor:0.7 nM (ki)|SST2 receptor:4720 nM (ki)|SST1 receptor:199 nM (ki)|SST5 receptor:3880 nM (ki)
• 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).
• In Vitro:
  L-803087 has Ki values of 199, 4720, 1280, and 3880 nM for cloned human sst1, sst2, sst3, and sst5 receptors, respectively. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

L 803087, L803087, L-803087, sst5 receptor, sst2 receptor, sst3 receptor, sst4 receptor, SST1, sst1 receptor

Compound Identifiers

PubChem CID

5311374