產品屬性：
產品名稱 | PF-04859989 (hydrochloride) |
規格 | 1 mg、5 mg、10 mg、25 mg |
貨號 | EY-01Y13515 |
Cas No.: 177943-33-8
別名: N/A
化學名: N/A
分子式: C9H10N2O2.HCl
分子量: 214.7
溶解度: DMSO: 22 mg/ml,Water: 22 mg/ml
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
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).1 It 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.21.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)
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