GP3269
CAS No. : 186393-42-0
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| Cat. No. : | HY-19259 |
| M.Wt: | 420.44 |
| Formula: | C23H21FN4O3 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
In Vitro:GP3269 (20 minutes at 37 °C) potently inhibits purified pig heart adenosine kinase with an IC50 of 11 nM[1].
In Vivo: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].
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