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CYM2503

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Catalog No. T8963Cas No. 1308833-36-4

CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own).

CYM2503

CYM2503

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Purity: 97.04%
Catalog No. T8963Cas No. 1308833-36-4
CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
5 mg$73In StockIn Stock
10 mg$118In StockIn Stock
25 mg$238In StockIn Stock
50 mg$382In StockIn Stock
100 mg$538In StockIn Stock
200 mg$733In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:97.04%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own).
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.
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.
Chemical Properties
Molecular Weight777.95
FormulaC45H55N5O7
Cas No.1308833-36-4
SmilesCc1cc(=O)[nH]c2cc(NC(=O)[C@H](CCCNC(=O)OC(C)(C)C)NC(=O)[C@H](CC3CCCCC3)NC(=O)OCC3c4ccccc4-c4ccccc34)ccc12
Relative Density.1.210 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (64.27 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.2854 mL6.4271 mL12.8543 mL64.2715 mL
5 mM0.2571 mL1.2854 mL2.5709 mL12.8543 mL
10 mM0.1285 mL0.6427 mL1.2854 mL6.4271 mL
20 mM0.0643 mL0.3214 mL0.6427 mL3.2136 mL
50 mM0.0257 mL0.1285 mL0.2571 mL1.2854 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

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All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
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