LY344864

SKU: orb1223215

Description

LY344864 is a selective 5-HT1F receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. LY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined. LY344864 was shown to be a full agonist producing an effect similar in magnitude to serotonin itself.

Key Properties

• CAS Number: 186544-26-3
• MW: 351.42
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₂FN₃O
• SMILES: CN(C)[C@@H]1CCc2c(C1)c1c([nH]2)ccc(c1)NC(=O)c1ccc(cc1)F.Cl
• Target: FGFR
• Solubility: DMSO : ≥ 350 mg/mL; 995.96 mM

Bioactivity

• In Vivo:
  LY 344864 (0-10 ng/kg; p.o. or i. v. ; once) inhibits neurogenic dural inflammation in rat migraine pain model. LY 344864 (1 mg/kg; i. v. ; once) can cross the blood brain barrier to some extent in rats. LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improved behavioral endpoints in a Parkinson’s disease mouse model. Animal model: Male Wistar rats, migraine pain model. Dosage: 1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous). Administration: Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation. Result: When given intravenously 10 minutes before stimulation, inhibited inflammation with an ID50 (median infective dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal stimulation, an ID50 of 1.2 ng/kg was obtained. Animal model: Male C57BL/6 mice, Parkinson’s disease model. Dosage: 2 mg/kg. Administration: Intraperitoneal injection, daily for 14d beginning 7d post-lesion. Result: Attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals, also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect.
• In Vitro:
  LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, 5-HT7, rat α1-adrenergic, rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively. LY 344864 is a inducer of mitochondrial biogenesis.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY-344864 | LY344864 | LY-344864 HCl

Quick Database Links

Gene Symbol

FGFR