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CAS No.: 890655-80-8

Verdiperstat/维迪珀斯塔 Catalog No. CSN23721

Synonyms: AZD3241;CAS#890655-80-8

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

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技术信息

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 C_max 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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9476 mL
- 19.7379 mL
- 39.4758 mL
- 5 mM
- 0.7895 mL
- 3.9476 mL
- 7.8952 mL
- 10 mM
- 0.3948 mL
- 1.9738 mL
- 3.9476 mL

技术信息

CAS号

890655-80-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H15N3O2S

运输

蓝冰

分子量

253.32

别名

AZD3241;CAS#890655-80-8

溶解度

DMSO	51.0 mg/mL (201.3 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (39.5 mM)

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