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VU 0365114

Cat. No. M7472
VU 0365114 Structure
Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 150  USD150 In stock
25mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

VU 0365114 is a selective positive allosteric modulator of M5 (EC50 values are 2.7 μM for human M5, and >30 μM for M1, M2, M3 and M4 receptors).

Chemical Information
Molecular Weight 397.35
Formula C22H14F3NO3
CAS Number 1208222-39-2
Solubility (25°C) DMSO 39 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] Schnee and Brown. J Pharmacol Exp Ther. Selectivity of linopirdine (DuP 966), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons.

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