CYM2503 | CAS#1308833-36-4 | GAL2 receptor Modulator

MedKoo Cat#: 531759 | Name: CYM-2503

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

CYM-2503

CAS#1308833-36-4

Theoretical Analysis

MedKoo Cat#: 531759

Name: CYM-2503

CAS#: 1308833-36-4

Chemical Formula: C45H55N5O7

Exact Mass: 777.4101

Molecular Weight: 777.96

Elemental Analysis: C, 69.48; H, 7.13; N, 9.00; O, 14.40

Price and Availability

Size	Price	Availability
5mg	USD 120.00	Ready to ship
10mg	USD 190.00	Ready to ship
25mg	USD 350.00	Ready to ship
50mg	USD 550.00	Ready to ship
100mg	USD 950.00	Ready to ship
200mg	USD 1,650.00	Ready to ship

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Related CAS #

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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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#T22D03P09

QC Data

View QC data: current batch, Lot#T22D03P09

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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/

Preparing Stock Solutions

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:

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. PubMed PMID: 20660766; PubMed Central PMCID: PMC2930524.