Biological Activity
Potent metabotropic glutamate mGlu1 receptor antagonist (IC50 = 6.3 μM at rat mGlu1a). Displays ≥ 40-fold selectivity over other receptors: mGlu5, mGlu2, mGlu4a (IC50 > 300 μM), NMDA and AMPA (IC50 = 250 μM). Neuroprotective in cultured murine cortical cells and rat hippocampal slice cultures in vitro. Reduces the volume of ischemia-induced brain infarcts in rats following systemic administration in vivo.
Technical Data
M. Wt | 215.23 |
Formula | C8H9NO4S |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 518357-51-2 |
PubChem ID | 10398360 |
InChI Key | KOMWRBFEDDEWEP-UHFFFAOYSA-N |
Smiles | CC1=C(SC(=C1)C(O)=O)C(N)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
1eq. NaOH | 21.52 | 100 | |
DMSO | 10.76 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 215.23. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 4.65 mL | 23.23 mL | 46.46 mL |
5 mM | 0.93 mL | 4.65 mL | 9.29 mL |
10 mM | 0.46 mL | 2.32 mL | 4.65 mL |
50 mM | 0.09 mL | 0.46 mL | 0.93 mL |
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References
References are publications that support the products' biological activity.
Moroni et al (2002) The novel and systemically active metabotropic glutamate 1 (mGlu1) receptor antagonist 3-MATIDA reduces post-ischemic neuronal death. Neuropharmacology 42 741 PMID: 12015200
Cozzi et al (2002) Metabotropic glutamate 1 (mGlu1) receptor antagonists enhance GABAergic neurotransmission: a mechanism for the attenuation of post-ischemic injury and epileptiform activity? Neuropharmacology 43 119 PMID: 12213266
Constantino et al (2004) Stereoselective synthesis and preliminary evaluation of (+)- and (-)-3-methyl-5-carboxy-thien-2-yl-glycine (3-MATIDA): identification of (+)-3-MATIDA as a novel mGluR1 competitive antagonist. Il Farmaco 59 93 PMID: 14871500
Keywords: 3-MATIDA, supplier, Potent, selective, mGlu1, mGluR1, antagonists, mGlur, Group, I, Receptors, mGlu5, mGluR5, Glutamate, Metabotropic, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience