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PF-04859989 HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-04859989 HCl图片
CAS NO:177943-33-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
PF-04859989
PF-04859989HCl
PF04859989
PF 04859989
产品介绍
PF-04859989 HCl 是不可逆的犬尿氨酸转氨酶KAT II抑制剂,可透过血脑屏障,抑制 hKATⅡ 和 rKATⅡ 的IC50分别为 23 和 263 nM。它对 KATⅡ 的选择性高于人 KATⅠ、KATⅢ 和 KATⅣ (IC50分别为22、11和 >50 μM)。

产品描述

PF-04859989 HCl is a brain-penetrable and irreversible inhibitor of kynurenine amino transferase II (KAT II), which is the enzyme responsible for most of the brain synthesis of kynurenic acid.

体外活性

The IC50s values are 23 and 263 nM for hKAT II and rKAT II. PF-04859989 HCl is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[3].

体内活性

Acute administration of the KAT II inhibitor PF-04859989 (5 or 10 mg/kg) was associated with a short-onset, time-dependent decrease in firing rate and burst activity of DA neurons, both parameters reaching a 50% reduction within 45 min. Furthermore, PF-04859989 reduced the number of spontaneously active DA cells as measured 4-6 after administration. Pretreatment with d-cycloserine (30 mg/kg) or CGP-52432 (10 mg/kg) prevented the inhibitory action of PF-04859989 (5 mg/kg) on firing rate and burst firing activity. In contrast, pretreatment with methyllycaconitine (MLA, 4 mg/kg) did not change the response, whereas picrotoxin (4.5 mg/kg) partially prevented the inhibitory effects of PF-04859989 (5 mg/kg, i.v.)[2].

Cas No.

177943-33-8

分子式

C9H11ClN2O2

分子量

214.65

别名

PF-04859989;PF-04859989HCl;PF04859989;PF 04859989;PF-04859989 HCl

储存和溶解度

DMSO:100 mg/mL (465.87 mM)
H2O:100 mg/mL (465.87 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years