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CYM2503

🥰Excellent
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

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg$31In Stock
5 mg$73In Stock
10 mg$118In Stock
25 mg$238In Stock
50 mg$382In Stock
100 mg$538In Stock
200 mg$733In Stock
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Purity:97.04%
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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.
Solubility Information
DMSO: 50 mg/mL (64.27 mM)
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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