VU 0467485

Name: VU 0467485
Brand: Tocris Bioscience
SKU: 6932
Price: 231 USD

Catalog # 6932 | Tocris Bioscience a Bio-Techne Brand

COA / SDS

Potent and selective positive allosteric modulator of M4 receptors; orally bioavailable and brain penetrant

Key Product Details

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)
Molecular Weight:	360.41

View Full Technical Details for VU 0467485

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 M_{1-3, 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.

Solubility for VU 0467485

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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 Discovery of VU0467485/AZ13713945: an M₄ PAM evaluated as a preclinical candidate for the treatment of schizophrenia. ACS Med.Chem.Lett. 2016 PMID: 28197318

Citations for VU 0467485

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