购物车
- 全部删除
- 您的购物车当前为空
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)。
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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 247 | 现货 | |
5 mg | ¥ 496 | 现货 | |
10 mg | ¥ 762 | 现货 | |
25 mg | ¥ 1,490 | 现货 | |
50 mg | ¥ 2,360 | 现货 | |
100 mg | ¥ 2,970 | 现货 | |
500 mg | ¥ 6,920 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 488 | 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-04859989HCl, PF-04859989, PF04859989, PF 04859989 |
分子量 | 214.65 |
分子式 | C9H11ClN2O2 |
CAS No. | 177943-33-8 |
Smiles | Cl.N[C@H]1Cc2ccccc2N(O)C1=O |
密度 | 1.31g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (465.87 mM) H2O: 100 mg/mL (465.87 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/H2O
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容