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MDL 29951 (CAS 130798-51-5) LS-H124

NMDA receptor antagonist
LS-H124-500 / 500 µg / $195
LS-H124-1000 / 1000 µg / $225
LS-H124-5000 / 5000 µg / $295
LS-H124-10000 / 10000 µg / $405
USA Shipment Only
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Description: NMDA receptors are neuroreceptors that have binding sites for glycine or D-serine as well as L-glutamate. MDL 29951 is an antagonist of NMDA receptors with high affinity for the glycine binding site (Ki = 140 nM). It is functional both in vitro and in vivo. MDL 29951 blocks NMDA receptor-dependent convulsions in audiogenic seizure-susceptible DBA/2J mice. It is used to evaluate the role of the glycine site of the NMDA receptor in neurological signaling. MDL 29951 is also an agonist of the G protein-coupled receptor GPR17 (EC50 values range from 7 nM to 6 µM, depending on the assay). GPR17 is thought to be involved in oligodendrocyte differentiation and myelin formation/repair. H124_ChemicalStructureImage.png
2-?carboxy-?4,?6-?dichloro-1H-?indole-?3-?propanoic acid
 
biochemical, chemical, antagonist
LS-H124
130798-51-5
C12H9Cl2NO4
≥98%
A crystalline solid
 
ClC1=CC(Cl)=C(C(CCC(O)=O)=C(C(O)=O)N2)C2=C1
InChI=1S/C12H9Cl2NO4/c13-5-3-7(14)10-6(1-2-9(16)17)11(12(18)19)15-8(10)4-5/h3-4,15H,1-2H2,(H,16,17)(H,18,19)
KNBSYZNKEAWABY-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: GRIN1 / NMDAR1 related products

Usage Information

MDL 29951 is supplied as a crystalline solid. A stock solution may be made by dissolving the MDL 29951 in the solvent of choice. MDL 29951 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of MDL 29951 in these solvents is approximately 0.25, 10, and 5 mg/ml, repsectively. MDL 29951 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, MDL 29951 should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. MDL 29951 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Karakas, E. and Furukawa, H. Crystal structure of a heterotetrameric NMDA receptor ion channel. Science 344(6187), 992-997 (2014).
  2. Baron, B.M., Harrison, B.L., McDonald, I.A., et al. Potent indole- and quinoline-containing N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site. J. Pharmacol. Exp. Ther. 262, 947-956 (1992).
  3. Millan, M.J. and Seguin, L. Chemically-diverse ligands at the glycine B site coupled to N-methyl-D-aspartate (NMDA) receptors selectively block the late phase of formalin-induced pain in mice. Neurosci. Lett. 178, 139-143 (1994).
  4. Heppenstall, P.A. and Fleetwood-Walker, S.M. The glycine site of the NMDA receptor contributes to neurokinin1 receptor agonist facilitation of NMDA receptor agonist-evoked activity in rat dorsal horn neurons. Brain Res. 744, 235-245 (1997).
  5. Hennen, S., Wang, H., Peters, L., et al. Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist. Sci. Signal. 6(298), 2-16 (2013).

 


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