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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.
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|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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.
View all Glutamate (Metabotropic) Group I Receptor Modulators
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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