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首页 / 抑制剂/激动剂 / 其他抑制剂/激动剂 /
其他
MPO
/ Verdiperstat

维迪珀斯塔 /Verdiperstat {[allProObj[0].p_purity_real_show]}

货号：A1001768 同义名： AZD 3241;BHV-3241

Verdiperstat is a potent, reversible and orally active myeloperoxidase (MPO) selective inhibitor with IC50 of 630 nM.

Verdiperstat 化学结构 CAS号：890655-80-8
Verdiperstat 化学结构
CAS号：890655-80-8
Verdiperstat 3D分子结构
CAS号：890655-80-8
Verdiperstat 化学结构 CAS号：890655-80-8
Verdiperstat 3D分子结构 CAS号：890655-80-8
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Verdiperstat 纯度/质量文件 产品仅供科研

货号：A1001768 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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Verdiperstat 生物活性

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].

Verdiperstat 参考文献

[1]Johnström P, Bergman L, Varnäs K, Malmquist J, Halldin C, Farde L. Development of rapid multistep carbon-11 radiosynthesis of the myeloperoxidase inhibitor AZD3241 to assess brain exposure by PET microdosing. Nucl Med Biol. 2015;42(6):555-560.

[2]Jucaite A, Svenningsson P, Rinne JO, et al. Effect of the myeloperoxidase inhibitor AZD3241 on microglia: a PET study in Parkinson's disease. Brain. 2015;138(Pt 9):2687-2700.

Verdiperstat 实验方案

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

Verdiperstat 技术信息

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

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
溶解度

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
动物实验配方

Tags: Verdiperstat | 890655-80-8 | AZD3241 | AZD 3241 | AZD-3241 | Glutathione Peroxidase | MPO Inhibitor | Apoptosis | Metabolic Enzyme/Protease | Glutathione Peroxidase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Verdiperstat 纯度/质量文件 | Verdiperstat 生物活性 | Verdiperstat 参考文献 | Verdiperstat 实验方案 | Verdiperstat 技术信息

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