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CYM2503

Chemical Structure : CYM2503

CAS No.: 1308833-36-4

CYM2503 (CYM 2503)

Catalog No.: PC-38482Not For Human Use, Lab Use Only.

CYM2503 is a putative galanin receptors type 2 (GalR2) positive allosteric modulator, concentration-dependently potentiates galanin (100 nM) stimulated IP1 accumulation in HEK293-GalR2 cells with EC50 of 0.69 uM, efficacy of 9.7-fold potentiation.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CYM2503 is a putative galanin receptor type 2 (GalR2) positive allosteric modulator, concentration-dependently potentiates galanin (100 nM) stimulated IP1 accumulation in HEK293-GalR2 cells with EC50 of 0.69 uM, efficacy of 9.7-fold potentiation.
CYM2503 exhibited no affinity for GalR1 anddid not modulate GalR1 signaling.
CYM2503 mediated potentiation of the agonist-stimulated GalR2 activation and the lack of affinity of CYM2503 for GalR2 orthosteric site in HEK293-GalR2 cells.
CYM2503 increased the latency to first electrographic seizure and the latency to first stage 3 behavioral seizure, decreased the latency to the establishment of SE, and dramatically decreased mortality in the rat Li-pilocarpine SE model.
CYM2503 increased the latency to first electrographic seizure and decreased the total time in seizure in Li-pilocarpine seizure model in mice, also attenuated electroshock-induced seizures in mice.

Physicochemical Properties

M.Wt 777.96
Formula C45H55N5O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

tert-butyl ((S)-5-((S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3-cyclohexylpropanamido)-6-((4-methyl-2-oxo-1,2-dihydroquinolin-7-yl)amino)-6-oxohexyl)carbamate

References

1. Xiaoying Lu, et al. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34.

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