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TASP0433864 

Cat. No. M28422
TASP0433864  Structure
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Biological Activity

TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity.

Chemical Information
Molecular Weight 329.39
Formula C18H23N3O3
CAS Number 1431980-60-7
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] Tetsuaki Hiyoshi, et al. J Pharmacol Exp Ther. Neurophysiologic and antipsychotic profiles of TASP0433864, a novel positive allosteric modulator of metabotropic glutamate 2 receptor

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  Catalog
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Keywords: TASP0433864  supplier, GluR, inhibitors, activators


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