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Submit ReviewVU 0409551
Description: Selective positive allosteric modulator of mGlu5 receptors; brain penetrant and orally bioavailable
Alternative Names: JNJ 46778212
Chemical Name: [6,7-Dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](fluorophenyl)methanone
Purity: ≥98% (HPLC)
Biological Activity for VU 0409551
VU 0409551 is a 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.
Compound Libraries for VU 0409551
VU 0409551 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for VU 0409551
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VU 0409551
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.24 | 100 | |
| ethanol | 17.62 | 50 |
Preparing Stock Solutions for VU 0409551
The following data is based on the product molecular weight 352.36. 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 | 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 for VU 0409551
References for VU 0409551
References are publications that support the biological activity of the product.
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
Ghoshal et al (2017) Role of mGlu5 receptors and inhibitory neurotransmission in M1 dependent muscarinic LTD in the prefrontal cortex: implications in Schizophrenia. ACS Chem.Neurosci. 8 2254 PMID: 28679049
If you know of a relevant reference for VU 0409551, please let us know.
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Keywords: VU 0409551, VU 0409551 supplier, JNJ46778212, VU0409551, metabotropic, glutamate, receptors, mGlu5, positive, allosteric, modulators, modulates, PAMs, JNJ, 46778212, Glutamate, (Metabotropic), Group, I, Receptors, 5693, Tocris Bioscience
Citations for VU 0409551
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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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