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VU 0155041 sodium salt

Cat. No. M7468
VU 0155041 sodium salt Structure
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Biological Activity

VU 0155041 sodium salt is a potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively). Active in in vivo models of Parkinson's disease following i.c.v. administration.

Chemical Information
Molecular Weight 338.16
Formula C14H14Cl2NNaO3
CAS Number 1259372-69-4
Solubility (25°C) Water 8.45 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] He, et al. J Pharmacol Exp Ther. A role for tryptase in the activation of human mast cells: modulation of histamine release by tryptase and inhibitors of tryptase.

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