MPO-IN-28

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Chemical Structure| 37836-90-1 同义名 : -
CAS号 : 37836-90-1
货号 : A1148094
分子式 : C11H13N5O
纯度 : 98%
分子量 : 231.254
MDL号 : MFCD00475732
存储条件:

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 12 mg/mL(51.89 mM),配合低频超声,并水浴加热至45℃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 The heme enzyme myeloperoxidase (MPO) participates in innate immune defense mechanism through formation of microbicidal reactive oxidants. MPO-IN-28 is a the first potent, selective and mechanism-based irreversible MPO inhibitor with IC50 value of 44nM. MPO-IN-28 achieved residual MPO activity without H2O2 by 84%, residual MPO activity with H2O2 by 4%, residual MPO activity with Cl+ H2O2 by 5% at 5μM and inhibited LDL oxidation with IC50 value of 0.09μM. It dose-dependently inhibited MPO inside neutrophils with IC50 value of 93.1μM. MPO-IN-28 possesses the characteristic of blood−brain barrier permeability, human intestinal absorption and cell permeability. It inhibited in vitro growth of normal human dermal fibroblast with IC50 value 17μM[2].
作用机制 MPO-IN-28 interacts with the active site of MPO and MPO uses hydrogen peroxide to oxidize MPO-IN-28 thereby irreversibly inactivating the enzyme.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.32mL

0.86mL

0.43mL

21.62mL

4.32mL

2.16mL

43.24mL

8.65mL

4.32mL

参考文献

[1]Soubhye J, Chikh Alard I, et al. Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. J Med Chem. 2017 Aug 10;60(15):6563-6586.

[2]Soubhye J, Chikh Alard I, Aldib I, Prévost M, Gelbcke M, De Carvalho A, Furtmüller PG, Obinger C, Flemmig J, Tadrent S, Meyer F, Rousseau A, Nève J, Mathieu V, Zouaoui Boudjeltia K, Dufrasne F, Van Antwerpen P. Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. J Med Chem. 2017 Aug 10;60(15):6563-6586. doi: 10.1021/acs.jmedchem.7b00285. Epub 2017 Jul 19. PMID: 28671460.