CYM2503

SKU: orb1298487

Description

CYM2503 is a selective positive allosteric modulator (PAM) of the GAL2 receptor, enhancing galanin-mediated IP1 accumulation without orthosteric binding or intrinsic activity. This tool compound is useful for studying galaninergic signaling in neuropharmacology research, including investigations into pain, mood, and feeding behavior in vitro and in vivo.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1308833-36-4
• MW: 777.95
• Purity: 97.04% (May vary between batches)
• Formula: C₄₅H₅₅N₅O₇
• SMILES: Cc1cc(=O)[nH]c2cc(NC(=O)[C@H](CCCNC(=O)OC(C)(C)C)NC(=O)[C@H](CC3CCCCC3)NC(=O)OCC3c4ccccc4-c4ccccc34)ccc12
• Target: Neuropeptide Y Receptor
• Solubility: DMSO:50 mg/mL (64.27 mM)

Bioactivity

• In Vivo:
  In the rat Li-pilocarpine status epilepticus model, CYM2503, injected intraperitoneally, increased the latency to first electrographic seizure and the latency to first stage 3 behavioral seizure, decreased the latency to the establishment of status epilepticus, and dramatically decreased the mortality. In a Li-pilocarpine seizure model in mice, CYM2503 increased the latency to first electrographic seizure and decreased the total time in seizure. CYM2503 also attenuated electroshock-induced seizures in mice. Thus, CYM2503 provides a starting point for the development of anticonvulsant therapy using the galanin R2 receptor as target.
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• In Vitro:
  CYM2503 potentiated the galanin-stimulated IP1 accumulation in HEK293 cells stably expressing GalR2 receptor, whereas it exhibited no detectable affinity for the (125)I galanin-binding site of GalR2 receptor, an effect consistent with that of a positive allosteric modulator.
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Storage & Handling

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

Alternative Names

Neuropeptide Y Receptor, NeuropeptideYReceptor, NPY receptor, inhibit, Inhibitor, GAL2, GalR2, electrographic seizure, epilepsy, CYM 2503, CYM2503, CYM-2503, seizure

Compound Identifiers

PubChem CID

68045954