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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)
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 |
| 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.
Product Datasheets for VU 0467485
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
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