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Description: Selective positive allosteric modulator of mGlu2 receptors
Chemical Name: (2S)-2-[[4-(1,1-Dimethylethyl)phenoxy]methyl]-2,3-dihydro-5-methylimidazo[2,1-b]oxazole-6-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for TASP 0433864
TASP 0433864 is a 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.
Compound Libraries for TASP 0433864
TASP 0433864 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for TASP 0433864
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TASP 0433864
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.94 | 100 | |
| ethanol | 6.59 | 20 |
Preparing Stock Solutions for TASP 0433864
The following data is based on the product molecular weight 329.39. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for TASP 0433864
References for TASP 0433864
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TASP 0433864, please let us know.
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Keywords: TASP 0433864, TASP 0433864 supplier, TASP0433864, metabotropic, glutamate, receptors, 2, positive, allosteric, modulators, modulates, mGlu2, mGluR, selective, PAM, Glutamate, (Metabotropic), Group, II, Receptors, 5362, Tocris Bioscience
Citations for TASP 0433864
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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