PF-04859989 (hydrochloride) 是一种脑渗透性、不可逆的犬尿氨酸氨基转移酶 (KAT) II 抑制剂，对 hKAT II 和 rKAT II 的 IC50 分别为 23 和 263 nM。
货号:ajcx23260
CAS:177943-33-8
分子式:C9H10N2O2.HCl
分子量：214.7
溶解度:DMSO: 22 mg/ml,Water: 22 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC₅₀s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).¹It is selective for KAT II over KAT I, -III, and -IV (IC₅₀s = 21.6, 107, and >50 µM, respectively).In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC₅₀= 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.²

1.Kozak, R., Campbell, B.M., Strick, C.A., et al.Reduction of brain kynurenic acid improves cognitive functionJ. Neurosci.34(32)10592-10602(2014) 2.Yoshida, T., Yamasaki, S., Kaneko, O., et al.A covalent small molecule inhibitor of glutamate-oxaloacetate transaminase 1 impairs pancreatic cancer growthBiochem. Biophys. Res. Commun.522(3)633-638(2020)