VU 0467485

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Description: Potent and selective positive allosteric modulator of M4 receptors; orally bioavailable and brain penetrant
Chemical Name: 5-Amino-N-[(3-fluoro-4-methoxyphenyl)methyl]-3,4-dimethylthieno[2,3-c]pyridazine-6-carboxamide
Purity: ≥98% (HPLC)
Literature (2)

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.

Licensing Information

Sold under license from Vanderbilt University.

Technical Data for VU 0467485

M. Wt 360.41
Formula C17H17FN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1451994-10-7
PubChem ID 89777239
Smiles COC1=C(C=C(C=C1)CNC(C2=C(C3=C(C(C)=NN=C3S2)C)N)=O)F

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
DMSO 7.21 20

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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

If you know of a relevant reference for VU 0467485, please let us know.

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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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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.