Verdiperstat

产品说明书

Print
Chemical Structure| 890655-80-8 同义名 : AZD 3241;BHV-3241;CAS#890655-80-8.
CAS号 : 890655-80-8
货号 : A1001768
分子式 : C11H15N3O2S
纯度 : 99%+
分子量 : 253.321
MDL号 : MFCD30533444
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.