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Biological Activity for VU 0467485
VU 0467485 is a potent and selective positive allosteric modulator of M4 receptor; potentiates activity of ACh at M4 (EC50 values are 26.6 and 78.8 nM at rat and human M4 receptors, respectively). Exhibits selectivity for M4 over human and rat M1-3, 5, and a panel of 200 other pharmacological targets. Displays efficacy in a rat model of antipsychotic activity. Orally bioavailable and brain penetrant.
Sold under license from Vanderbilt University.
Technical Data for VU 0467485
|Storage||Store at -20°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.
Solubility Data for VU 0467485
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for VU 0467485
The following data is based on the product molecular weight 360.41. 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|
|0.2 mM||13.87 mL||69.37 mL||138.73 mL|
|1 mM||2.77 mL||13.87 mL||27.75 mL|
|2 mM||1.39 mL||6.94 mL||13.87 mL|
|10 mM||0.28 mL||1.39 mL||2.77 mL|
References for VU 0467485
References are publications that support the biological activity of the product.
Wood et al (2016) Discovery of VU0467485/AZ13713945: an M4 PAM evaluated as a preclinical candidate for the treatment of schizophrenia. ACS Med.Chem.Lett. 8 233 PMID: 28197318
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Keywords: VU 0467485, VU 0467485 supplier, VU0467485, positive, allosteric, modulators, selective, acetycholine, muscarinic, receptors, M4, antipsychotic, orally, bioavailable, Receptors, 6932, Tocris Bioscience
Citations for VU 0467485
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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!
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.