货号:A1001768 同义名: AZD 3241;BHV-3241
Verdiperstat是一种强效、可逆、口服活性的髓过氧化物酶(MPO)选择性抑制剂,IC50 为 630 nM,可用于神经退行性疾病研究。
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描述 | Myeloperoxidase (MPO) is a heme-containing peroxidase that contributes to the microbicidal activity of neutrophils and monocytes through the generation of reactive oxidants such as hypochlorous acid. Accumulating evidence suggest that excessive generation of MPO-derived oxidants is linked to tissue damage in many diseases, especially those characterized by acute or chronic inflammation. AZD3241 (Verdiperstat) inhibits the human MPO enzyme with an IC50 of 630 nM. After iv injection of [11C]AZD3241 there was a rapid presence of radioactivity in brain in each of the three monkeys. The distribution of [11C]AZD3241 to brain was fast and a Cmax of 1.9% to 2.6% of the injected radioactivity was observed within 1.5 min and followed by a rapid wash-out of radioactivity to about 0.4% at 60 min[1]. In parkinson patients (n = 18) receving either AZD3241 600 mg orally twice a day or placebo (in 3:1 ratio) for 8 weeks, the total distribution volume of 11C-PBR28 binding to translocator protein was significantly reduced compared to baseline both at 4 and 8 weeks (P < 0.05). The distribution volume reduction across nigrostriatal regions at 8 weeks ranged from 13-16%, with an effect size equal to 0.5-0.6[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.95mL 0.79mL 0.39mL |
19.74mL 3.95mL 1.97mL |
39.48mL 7.90mL 3.95mL |
CAS号 | 890655-80-8 |
分子式 | C11H15N3O2S |
分子量 | 253.321 |
别名 | AZD 3241;BHV-3241;CAS#890655-80-8. |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,2-8°C |
溶解方案 |
DMSO: 120 mg/mL(473.71 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |