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VU 0155041

Cat. No. M7467
VU 0155041 Structure
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Biological Activity

VU 0155041 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. Also available as sodium salt (Cat. No. 3311).

Chemical Information
Molecular Weight 316.18
Formula C14H15Cl2NO3
CAS Number 1093757-42-6
Solubility (25°C) 1eq. NaOH 31.62 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] Chiellini, et al. Chem Biol. A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.

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