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Adenosine receptor inhibitor 2

Cat. No. M40661
Adenosine receptor inhibitor 2 Structure
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Biological Activity

Adenosine receptor inhibitor 2 is a potent adenosine receptor AR inhibitor with dual affinity for A1/A2A ARs with Ki values of 52.2 and 167 nM, respectively.

Chemical Information
Molecular Weight 406.28
Formula C17H20BrN5O2
CAS Number 2550401-76-6
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] Helena Marcelino et al. J Neurochem. Adenosine inhibits human astrocyte proliferation independently of adenosine receptor activation

[2] Amirhossein Bahreyni et al. J Pharm Pharmacol. Therapeutic potency of pharmacological adenosine receptor agonist/antagonist in angiogenesis, current status and perspectives

[3] Hillary A Johnston-Cox et al. J Cell Physiol. Physiological implications of adenosine receptor-mediated platelet aggregation

[4] Luo Yan et al. Expert Opin Emerg Drugs. Adenosine receptor agonists: from basic medicinal chemistry to clinical development

[5] Todd W Shearer et al. Invest Ophthalmol Vis Sci. Adenosine A1 receptor modulation of MMP-2 secretion by trabecular meshwork cells

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