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VU6001966 

Cat. No. M29103
VU6001966  Structure
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Biological Activity

VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer.

Chemical Information
Molecular Weight 326.33
Formula C17H15FN4O2
CAS Number 2009052-76-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gengyang Yuan, et al. J Med Chem. Synthesis and Characterization of 5-(2-Fluoro-4-[11C]methoxyphenyl)-2,2-dimethyl-3,4-dihydro-2 H-pyrano[2,3- b]pyridine-7-carboxamide as a PET Imaging Ligand for Metabotropic Glutamate Receptor 2

[2] Katrina A Bollinger, et al. ACS Med Chem Lett. Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core

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Keywords: VU6001966  supplier, GluR, inhibitors, activators


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