中文名 | 1,4-二氧代-2,3-二溴甲基喹啉 |
英文名 | 2,3-bis(bromomethyl)-1-oxoquinoxalin-1-ium-4(1H)-olate |
别名 | 1,4-二氧代-2,3-二溴甲基喹啉 1,4-二氧代-2,3-二溴甲基喹喔啉 |
英文别名 | Conoidin A 1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline 2,3-Bis-bromomethyl-quinoxaline 1,4-dioxide 2,3-bis(bromomethyl)quinoxaline-1,4-dioxide 2,3-BIS(BROMOMETHYL)QUINOXALINE 1,4-DIOXIDE Quinoxaline, 2,3-bis(bromomethyl)-, 1,4-dioxide quinoxaline, 2,3-bis(bromomethyl)-, 1,4-dioxide 2,3-bis(broMoMethyl)-1-oxoquinoxalin-1-iuM-4(1H)-olate 2,3-bis(bromomethyl)-1-oxoquinoxalin-1-ium-4(1H)-olate |
CAS | 18080-67-6 |
化学式 | C10H8Br2N2O2 |
分子量 | 347.99 |
InChI | InChI=1/C10H8Br2N2O2/c11-5-9-10(6-12)14(16)8-4-2-1-3-7(8)13(9)15/h1-4H,5-6H2 |
密度 | 1.95±0.1 g/cm3(Predicted) |
熔点 | 180-190 °C (decomp) |
沸点 | 512.3±60.0 °C(Predicted) |
酸度系数 | 1.91±0.30(Predicted) |
存储条件 | -20℃ |
靶点 | Toxoplasma gondii |
体外研究 | Peroxiredoxins are a widely conserved family of enzymes that function in antioxidant defense and signal transduction. And the changes in PrxII expression are associated with a variety of human diseases, including cancer.Conoidin A binds to the peroxidatic cysteine of TgPrxII, inhibiting its enzymatic activityin vitro. Conoidin A also shown to alkylate or crosslink catalytic cysteines of wild type AcePrx-1 inAncylostoma ceylanicumand human PrxII and PrxIV with similar efficiency. But it is ineffective to mitochondrial hPrxIII.Conoidin A (5 µM) can inhibit the glucose oxidase-mediated hyperoxidation of mammalian peroxiredoxin I and II. |
体内研究 | Conoidin A (intraperitoneal injection; 5mg/kg; for three successive days before MI/R injury) blocks the effect of Luteolin (HY-N0162) on the ST‐segment elevation.Furthermore, an increase in the infarct size presented of the MI/R group can be reduced by Luteolin. But pre‐treatment with conoidin A abolishs the effect of Luteolin. Pre‐treatment with conoidin A also prevents Luteolin-reduced activities of CK‐MB, AST and LDH in vivo . Animal Model: Rat myocardial I/R model Dosage: 5mg/kg Administration: Intraperitoneal injection; 5mg/kg; for three successive days before MI/R injury Result: Significantly reversed the antioxidative effect of Luteolin. Impaired the protective effects of luteolin. |
参考资料 展开查看 | 1. Jeralyn D Haraldsen, et al. IDENTIFICATION OF CONOIDIN A AS A COVALENT INHIBITOR OF PEROXIREDOXIN II. Org Biomol Chem. 2009;7:3040-3048.2. Gu Liu, et al. Optimisation of conoidin A, a peroxiredoxin inhibitor. ChemMedChem. 2010 Jan;5(1):41-5.3. Bo Wei, et al. Luteolin ameliorates rat myocardial ischaemia-reperfusion injury through activation of peroxiredoxin II. Br J Pharmacol |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.874 ml | 14.368 ml | 28.736 ml |
5 mM | 0.575 ml | 2.874 ml | 5.747 ml |
10 mM | 0.287 ml | 1.437 ml | 2.874 ml |
5 mM | 0.057 ml | 0.287 ml | 0.575 ml |
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