Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 296 | 现货 | ||
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,730 | 现货 | ||
50 mg | ¥ 2,820 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
200 mg | ¥ 5,330 | 现货 | ||
500 mg | ¥ 7,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 583 | 现货 |
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. |
靶点活性 | KAT II:23 nM(human), KAT II:263 nM(rat), KAT I:22 μM, KAT IV:>50 μM, KAT III:11 μM |
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]. |
别名 | PF 04859989, PF04859989, PF-04859989HCl, PF-04859989 |
分子量 | 214.65 |
分子式 | C9H11ClN2O2 |
CAS No. | 177943-33-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (465.87 mM)
H2O: 100 mg/mL (465.87 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 4.6587 mL | 23.2937 mL | 46.5875 mL | 116.4687 mL |
5 mM | 0.9317 mL | 4.6587 mL | 9.3175 mL | 23.2937 mL | |
10 mM | 0.4659 mL | 2.3294 mL | 4.6587 mL | 11.6469 mL | |
20 mM | 0.2329 mL | 1.1647 mL | 2.3294 mL | 5.8234 mL | |
50 mM | 0.0932 mL | 0.4659 mL | 0.9317 mL | 2.3294 mL | |
100 mM | 0.0466 mL | 0.2329 mL | 0.4659 mL | 1.1647 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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