GP3269 

GP3269 is a selective and orally active human adenosine kinase (AK) inhibitor with an IC₅₀ of 11 nM against human adenosine kinase. GP3269 increases adenosine levels at epileptic foci, activates A1 receptors on excitatory neurons, and exhibits anticonvulsant activity in rats. GP3269 does not induce hemodynamic effects including changes in blood pressure or heart rate in rats. GP3269 can be used for epilepsy-related research^[1].

GP3269 (20 minutes at 37 °C) potently inhibits purified pig heart adenosine kinase with an IC₅₀ of 11 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GP3269 (p.o.) suppresses seizures in the MES rat model with an ED₅₀ of 5.1 mg/kg^[1].
GP3269 has an oral bioavailability of 60% and a plasma half-life of 4.2 h in dogs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

420.44

C₂₃H₂₁FN₄O₃

186393-42-0

O[C@H]([C@@H]([C@H](O1)C)O)[C@]1([H])N2C3=NC=NC(NC4=CC=C(C=C4)F)=C3C(C5=CC=CC=C5)=C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Erion M D, et al. Design, synthesis and anticonvulsant activity of the potent adenosine kinase inhibitor GP3269. Nucleosides, Nucleotides & Nucleic Acids, 1997, 16(7-9): 1013-1021.