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A1AR antagonist 4

Cat. No. M40658
A1AR antagonist 4 Structure
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Biological Activity

A1AR antagonist 4 is a potent, selective adenosine receptor A1AR antagonist with a pIC50 of 5.51 and a pKi of 6.29.

Chemical Information
Molecular Weight 375.46
Formula C23H25N3O2
CAS Number 1031993-35-7
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] Eun Seon Pak et al. Kidney Res Clin Pract. Adenosine receptors as emerging therapeutic targets for diabetic kidney disease

[2] Christoph Eisner et al. Pflugers Arch. Profound hypothermia after adenosine kinase inhibition in A1AR-deficient mice suggests a receptor-independent effect of intracellular adenosine

[3] Marcus H Holschbach et al. Eur J Med Chem. Derivatives of 4,6-diamino-1,2-dihydro-2-phenyl-1,2,4-triazolo[4,3-a]quinoxalin-2H-1-one: potential antagonist ligands for imaging the A2A adenosine receptor by positron emission tomography (PET)

[4] F Da Settimo et al. J Med Chem. 3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists

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Keywords: A1AR antagonist 4 supplier, Adenosine Receptor, inhibitors, activators

 
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