Biological Activity
Selective mGlu5 positive allosteric modulator (EC50 = 260 nM). Selective for mGlu5 over other mGluR subtypes, as well as 66 other receptors and ion channels. Selectively potentiates mGlu5 signaling via Gαq. Exhibits wake-promoting, antipsychotic-like and cognition-enhancing effects in animal models. Brain penetrant and orally available.
Technical Data
| M. Wt | 352.36 |
| Formula | C20H17FN2O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1363281-27-9 |
| PubChem ID | 56846694 |
| InChI Key | QUZLMKNNIUSREV-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC=C(F)C=C1)N(C2)CCC3=C2OC(COC4=CC=CC=C4)=N3 |
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 | 35.24 | 100 | |
| ethanol | 17.62 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 352.36. 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 | 2.84 mL | 14.19 mL | 28.38 mL |
| 5 mM | 0.57 mL | 2.84 mL | 5.68 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.84 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Rook et al (2015) Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents. Neuron 86 1029 PMID: 25937172
Conde-Ceide et al (2015) Discovery of VU0409551/JNJ-46778212: An mGlu5 positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med.Chem.Lett. 6 716 PMID: 26157544
Keywords: VU 0409551, supplier, JNJ46778212, VU0409551, metabotropic, glutamate, receptors, mGlu5, positive, allosteric, modulators, modulates, PAMs, JNJ, 46778212, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
