VU 0467485

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Cat.No. 6932 - VU 0467485 | C17H17FN4O2S | CAS No. 1451994-10-7
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)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity

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

M. Wt 360.41
Formula C17H17FN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1451994-10-7
PubChem ID 89777239
InChI Key VFNHDIWHQGVWLL-UHFFFAOYSA-N
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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.21 20

Preparing Stock Solutions

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

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References

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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