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AR-R 17779 hydrochloride

Cat. No. M6464
AR-R 17779 hydrochloride Structure
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Biological Activity

AR-R 17779 hydrochloride is a selective agonist of α7 nAChRs (Ki values are 190 and 16000 nM for rat α7 and α4β2 receptors respectively). CNS penetrant after systemic administration.

Chemical Information
Molecular Weight 218.68
Formula C9H14N2O2.HCl
CAS Number 178419-42-6
Solubility (25°C) DMSO 10.93 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] Todde, et al. J Med Chem. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography.

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