WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H531759
CAS#: 1308833-36-4
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.
Hodoodo Cat#: H531759
Name: CYM-2503
CAS#: 1308833-36-4
Chemical Formula: C45H55N5O7
Exact Mass: 777.41
Molecular Weight: 777.960
Elemental Analysis: C, 69.48; H, 7.13; N, 9.00; O, 14.40
Synonym: CYM2503; CYM 2503; CYM-2503.
IUPAC/Chemical 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
InChi Key: BSFFWLJHCCBOPN-QARUCVQPSA-N
InChi Code: 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
SMILES Code: 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
Appearance: Solid powder
Purity: >96% (or refer to the Certificate of Analysis)
Shipping Condition: 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.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | CYM2503 is a putative GalR2-positive allosteric modulator. |
| 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/ |
The following data is based on the product molecular weight 777.96 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Lu X, Roberts E, Xia F, Sanchez-Alavez M, Liu T, Baldwin R, Wu S, Chang J, Wasterlain CG, Bartfai T. GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. doi: 10.1073/pnas.1008986107. Epub 2010 Jul 26. PMID: 20660766; PMCID: PMC2930524. |
| In vitro protocol: | 1. Lu X, Roberts E, Xia F, Sanchez-Alavez M, Liu T, Baldwin R, Wu S, Chang J, Wasterlain CG, Bartfai T. GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. doi: 10.1073/pnas.1008986107. Epub 2010 Jul 26. PMID: 20660766; PMCID: PMC2930524. |
| In vivo protocol: | 1. Lu X, Roberts E, Xia F, Sanchez-Alavez M, Liu T, Baldwin R, Wu S, Chang J, Wasterlain CG, Bartfai T. GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. doi: 10.1073/pnas.1008986107. Epub 2010 Jul 26. PMID: 20660766; PMCID: PMC2930524. |
1: Lu X, Roberts E, Xia F, Sanchez-Alavez M, Liu T, Baldwin R, Wu S, Chang J, Wasterlain CG, Bartfai T. GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15229-34. doi: 10.1073/pnas.1008986107. PubMed PMID: 20660766; PubMed Central PMCID: PMC2930524.
