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VU 0422288

Cat. No. M7474
VU 0422288 Structure
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Biological Activity

VU 0422288 is a group III mGlu receptor positive allosteric modulator (EC50 values are 108, 125 and 146 nM for mGlu4, mGlu8 and mGlu7 respectively). Exhibits selectivity over a panel of 68 other GPCRs, ion channels and transporters. Potentiates mGlu7-mediated reductions in excitatory post synaptic potentials in hippocampal slices.

Chemical Information
Molecular Weight 360.19
Formula C17H11Cl2N3O2
CAS Number 1630936-95-6
Solubility (25°C) DMSO 36.02 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Chen, et al. Neuroscience. Neuroprotective concentrations of the N-methyl-D-aspartate open-channel blocker memantine are effective without cytoplasmic vacuolation following post-ischemic administration and do not block maze learning or long-term potentiation.

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