An NMDA receptor antagonist and GPR17 agonist
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MDL 29951

Item No. 16266

Technical Information
Formal Name
2-carboxy-4,6-dichloro-1H-indole-3-propanoic acid
CAS Number
130798-51-5
Molecular Formula
C12H9Cl2NO4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
309 nm
SMILES
ClC1=CC(Cl)=C(C(CCC(O)=O)=C(C(O)=O)N2)C2=C1
InChi Code
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)
InChi Key
KNBSYZNKEAWABY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MDL 29951 is an antagonist of NMDA receptors with high affinity for the glycine binding site (Ki = 140 nM).1 It is functional both in vitro and in vivo.1 MDL 29951 blocks NMDA receptor-dependent convulsions in audiogenic seizure-susceptible DBA/2J mice.1 It is used to evaluate the role of the glycine site of the NMDA receptor in neurological signaling.2,3 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).4 GPR17 is thought to be involved in oligodendrocyte differentiation and myelin formation/repair.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Baron, B.M., Harrison, B.L., McDonald, I.A., et alPotent indole- and quinoline-containing N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site. J. Pharmacol. Exp. Ther. 262(3), 947-956 (1992).

    2. 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(1), 139-143 (1994).

    3. 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(2), 235-245 (1997).

    4. Hennen, S., Wang, H., Peters, L., et alDecoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist. Sci. Signal. 6(298), 2-16 (2013).