Galnon TFA

SKU: orb1298834

Description

Galnon is a small molecule, non-peptide agonist for galanin receptors, demonstrating selectivity for GAL1 (Ki=11.7 µM) over GAL2 (Ki=34.1 µM). It is a valuable research tool for studying galanin signaling in neurological processes, including pain, memory, and feeding behavior, in both cellular and animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1217448-19-5
• MW: 792.84
• Purity: 99.92% (May vary between batches)
• Formula: C₄₂H₄₇F₃N₄O₈
• SMILES: C(C(O)=O)(F)(F)F.C(OC(N[C@@H](CC1CCCCC1)C(N[C@H](C(NC=2C=C3C(=CC2)C(C)=CC(=O)O3)=O)CCCCN)=O)=O)C4C=5C(C=6C4=CC=CC6)=CC=CC5
• Target: Neuropeptide Y Receptor
• Solubility: DMSO:25 mg/mL (31.53 mM)

Bioactivity

• In Vivo:
  Galnon stimulated insulin release potently in isolated Wistar rat islets; 100 microM of the compound increased the release 8.5 times (p<0.001) at 3.3 mM and 3.7 times (p<0.001) at 16.7 mM glucose. Also in islet perifusions, galnon augmented several-fold both acute and late phases of insulin response to glucose. Furthermore, galnon stimulated insulin release in GK rat islets. These effects were not inhibited by the presence of galanin or the galanin receptor antagonist M35. The stimulatory effects of galnon were partly inhibited by the PKA and PKC inhibitors, H-89 and calphostin C, respectively, at 16.7 but not 3.3 mM glucose. In both Wistar and GK rat islets, insulin release was stimulated by depolarization of 30 mM KCl, and 100 microM galnon further enhanced insulin release 1.5-2 times (p<0.05). Cytosolic calcium levels, determined by fura-2, were increased in parallel with insulin release, and the L-type Ca2+-channel blocker nimodipine suppressed insulin response to glucose and galnon.galnon, a GAL receptor agonist, may enhance osteoclastic bone resorption in OVX rats. Although galnon reduced bone volume, biomechanical testing revealed that bone of galnon-treated animals was mechanically superior per unit area. Taken together, galnon simultaneously improves the intrinsic quality of cortical bone whilst stimulating osteoclastic activity in the OVX rat model.
• Animal Research:
  OVX rats were treated with either vehicle or galnon for 6 weeks via mini-osmotic pumps. Plasma osteocalcin concentrations, osseous cell gene expression, morphological and biomechanical properties of the skeleton were compared between the two groups

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

NeuropeptideYReceptor, Neuropeptide Y Receptor, GALNON TFA(475115 35 6(free base)), GALNON TFA(475115356(free base)), GALNON TFA(475115-35-6(free base)), galanin receptor

Compound Identifiers

PubChem CID

16219413