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WAY 181187 oxalate

Cat. No. M7482
WAY 181187 oxalate Structure
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Biological Activity

WAY 181187 oxalate is a high affinity and selective 5-HT6 agonist (Ki = 2.2 nM). Displays 60-fold selectivity over other 5-HT and monoamine receptors. Increases firing rate of 5-HT neurons. Modifies sleep and wakefulness profiles following direct injections into the dorsal raphe nucleus, in vivo. Orally bioavailable.

Chemical Information
Molecular Weight 470.91
Formula C15H13ClN4O2S2.C2H2O4
CAS Number 1883548-85-3
Solubility (25°C) DMSO 47.09 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] Brown, et al. J Neurochem. [3H]-Homoquinolinate binds to a subpopulation of NMDA receptors and to a novel binding site.

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