CYM-2503

• CAS: 1308833-36-4
• Catalog Number: ACM1308833364
• Category: Others
• Molecular Weight: 777.96
• Molecular Formula: C45H55N5O7
• Description: CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor which potentiates galanin-induced IP1 production 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.
• Synonyms: CYM2503; CYM 2503; CYM-2503
• IUPAC Name: 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
• Canonical SMILES: O=C(OC(C)(C)C)NCCCC[C@H](NC([C@@H](NC(OCC1C2=C(C3=C1C=CC=C3)C=CC=C2)=O)CC4CCCCC4)=O)C(NC5=CC6=C(C=C5)C(C)=CC(N6)=O)=O
• InChI: InChI=1S/C45H55N5O7/c1-28-24-40(51)48-38-26-30(21-22-31(28)38)47-41(52)37(20-12-13-23-46-43(54)57-45(2,3)4)49-42(53)39(25-29-14-6-5-7-15-29)50-44(55)56-27-36-34-18-10-8-16-32(34)33-17-9-11-19-35(33)36/h8-11,16-19,21-22,24,26,29,36-37,39H,5-7,12-15,20,23,25,27H2,1-4H3,(H,46,54)(H,47,52)(H,48,51)(H,49,53)(H,50,55)/t37-,39-/m0/s1
• InChI Key: BSFFWLJHCCBOPN-QARUCVQPSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: CYM2503 is a putative GalR2-positive allosteric modulator.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 69.48; H, 7.13; N, 9.00; O, 14.40
• Exact Mass: 777.4101
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: As shown in Fig. 2B, CYM2503 shifted the galanin concentration-response curve to the left. The EC50 was shifted by 50.4 ± 17.8-fold (mean ± SEM; n = 4), with 100 μM CYM2503. Smaller shifts of 12.5 ± 3.2-fold and 3.4 ± 0.7-fold were seen with 10 μM and 1 μM CYM2503, respectively. CYM2503 also increased the maximal galanin response by as much as 25 ± 9%.; Reference: Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. https://pubmed.ncbi.nlm.nih.gov/20660766/
• In Vivo Activity: Pretreatment with CYM2503 (15 min before pilocarpine) attenuated Li-pilocarpine-induced seizures in mice (Fig. 4). Overall, the effects of CYM2503 (60 mg/kg, i.p.) were comparable to those of levetiracetam (50 mg/kg i.p.) in this seizure model.; Reference: Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. https://pubmed.ncbi.nlm.nih.gov/20660766/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).