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ANR 94

Cat. No. M6445
ANR 94 Structure
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Biological Activity

ANR 94 is a adenosine A2A receptor (AA2AR) antagonist (Ki values are 643 and 46 nM for rat and human AA2ARs respectively). Most active AA2AR antagonist for human receptors. Displays activity in the treatment of Parkinson's disease in vivo; improves parkinsonian motor deficits and tremors. Exhibits neuroprotective and anti-inflammatory effects.

Chemical Information
Molecular Weight 207.23
Formula C9H13N5O
CAS Number 634924-89-3
Solubility (25°C) DMSO 10.36 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] Chang, et al. J Pharmacol Exp Ther. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A.

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