Biological Activity
Selective positive allosteric modulator at mGlu4 receptors (EC50 values are 240 and 110 nM at human and rat receptors respectively). Inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Brain penetrant.
Compound Libraries
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Technical Data
M. Wt | 262.69 |
Formula | C13H11ClN2O2 |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 1161205-04-4 |
PubChem ID | 44191096 |
InChI Key | ARYUXFNGXHNNDM-UHFFFAOYSA-N |
Smiles | ClC1=C(OC)C=C(NC(C2=NC=CC=C2)=O)C=C1 |
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 | |||
DMSO | 26.27 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 262.69. 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 | 3.81 mL | 19.03 mL | 38.07 mL |
5 mM | 0.76 mL | 3.81 mL | 7.61 mL |
10 mM | 0.38 mL | 1.9 mL | 3.81 mL |
50 mM | 0.08 mL | 0.38 mL | 0.76 mL |
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References
References are publications that support the products' biological activity.
Engers et al (2009) Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J.Med.Chem. 52 4115 PMID: 19469556
Engers et al (2011) Discovery, synthesis, and structure-activity relationship development of a series of N-(4-Acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu4) with CNS exposure in rats. J.Med.Chem. 54 1106 PMID: 21247167
Keywords: VU 0361737, supplier, Selective, positive, allosteric, modulators, mGlu4, mGluR4, group, III, metabotropic, glutamate, receptors, VU0361737, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Tocris Bioscience