Biological Activity
Selective mGlu2 receptor positive allosteric modulator (EC50 values are 199 and 206 nM for human and rat receptors, respectively). Exhibits negligible activity against a range of neurotransmitter targets, except 5-HT2B and MAO-B (72 and 92% inhibition at 10 μM, respectively). Potentiates inhibitory effect of DCG IV (Cat. No. 0975) on excitatory postsynaptic potentials in hippocampal slices and ketamine- and methamphetamine-induced increases in locomotor activity in rats and mice.
Technical Data
| M. Wt | 329.39 |
| Formula | C18H23N3O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1431980-60-7 |
| PubChem ID | 124201847 |
| InChI Key | IZYYTLCSQBACIP-AWEZNQCLSA-N |
| Smiles | CC(C)(C)C1=CC=C(OC[C@@H]2CN3C(O2)=NC(C(N)=O)=C3C)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 | 32.94 | 100 | |
| ethanol | 6.59 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 329.39. 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 | 3.04 mL | 15.18 mL | 30.36 mL |
| 5 mM | 0.61 mL | 3.04 mL | 6.07 mL |
| 10 mM | 0.3 mL | 1.52 mL | 3.04 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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References
References are publications that support the products' biological activity.
Hiyoshi et al (2014) Neurophysiologic and antipsychotic profiles of TASP0433864, a novel positive allosteric modulator of metabotropic glutamate 2 receptor. J.Pharmacol.Exp.Ther. 351 642 PMID: 25277141
Keywords: TASP 0433864, supplier, TASP0433864, metabotropic, glutamate, receptors, 2, positive, allosteric, modulators, modulates, mGlu2, mGluR, selective, PAM, Glutamate, (Metabotropic), Group, II, Receptors, Glutamate, (Metabotropic), Group, II, Receptors, Tocris Bioscience
