| Bioactivity | PF-04859989 is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[1]. |
| In Vivo | In vivo pharmacokinetic and efficacy studies in rat show that PF-04859989 is a brain-penetrant, irreversible inhibitor and is capable of reducing brain kynurenic acid by 50% at a dose of 10 mg/kg (sc)[1]. Rats receiving PF-04859989 (5 mg/kg; i.p.) exhibited a significantly lower number of spontaneously active DA neurons pertrack[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 34783-48-7 |
| Formula | C9H10N2O2 |
| Molar Mass | 178.19 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. "Amy B Dounay, et al. Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. ACS Med Chem Lett. 2012 Jan 25;3(3):187-92." [2]. Linderholm KR, et al. Inhibition of kynurenine aminotransferase II reduces activity of midbrain dopamine neurons. Neuropharmacology. 2016;102:42-47. |