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MRE3008F20 

Cat. No. M29697
MRE3008F20  Structure
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Biological Activity

MRE3008F20 is a highly efficient, highly selective and radioactive adenosine A3 receptor (AA3R) antagonist (Ki=1.8 nM). MRE3008F20 effectively antagonises Cl-IB-MECA-induced cAMP production in resting lymphocytes with an IC50 value of 5 nM. MRE3008F20 can be used in the study of AA3R.

Chemical Information
Molecular Weight 432.44
Formula C21H20N8O3
CAS Number 252979-43-4
Form Solid
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] Zhan-Guo Gao, et al. Purinergic Signal. Pharmacological characterization of DPTN and other selective A3 adenosine receptor antagonists

[2] Soo-Kyung Kim, et al. J Mol Graph Model. Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor

[3] Christa E Müller. Curr Top Med Chem. Medicinal chemistry of adenosine A3 receptor ligands

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  Catalog
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Keywords: MRE3008F20  supplier, Adenosine Receptor, inhibitors, activators


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