1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline
2,3-bis(bromomethyl)-1-oxoquinoxalin-1-ium-4(1H)-olate
CAS: 18080-67-6
Molecular Formula: C10H8Br2N2O2
1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline - Names and Identifiers
1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline - Physico-chemical Properties
| Molecular Formula | C10H8Br2N2O2 |
| Molar Mass | 347.99 |
| Density | 1.95±0.1 g/cm3(Predicted) |
| Melting Point | 180-190 °C (decomp) |
| Boling Point | 512.3±60.0 °C(Predicted) |
| pKa | 1.91±0.30(Predicted) |
| Storage Condition | -20℃ |
| Use | Conoidin A is a cell permeability inhibitor of Toxoplasma gondii peroxidase II (TgPrxII) and has nematicidal properties. Conoidin A covalently binds the TgPrxII peroxide catalytic site Cys47 to irreversibly inhibit its peroxide activity with an IC50 of 23 µM. Conoidin A also inhibits the oxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant and neuroprotective effects, and can be used in the study of ischemic heart disease. |
| Target | Toxoplasma gondii |
| In vitro study | 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. |
| In vivo study | 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. |
1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline - Reference
| Reference Show more | 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 |
1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
1,4-Dioxo-2,3-bis(bromomethyl)quinoxaline - Reference Information
| Biological activity | Conoidin A is a cell permeability inhibitor of Toxoplasma gondii peroxidase II (TgPrxII), which has the characteristics of killing nematodes. Conoidin A covalently binds the TgPrxII peroxide catalytic site Cys47 to irreversibly inhibit its peroxide activity with an IC50 of 23 µM. Conoidin A also inhibits the oxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant and neuroprotective effects, and can be used in the study of ischemic heart disease. |
| target | IC50: 23 µM ( T. gondii enzyme peroxiredoxin II (TgPrxII)) |
| in vitro study | Peroxiredoxins are a bright 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 show 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 m) can inhibit the glucose oxidase-mediated hyperoxidation of mammalian peroxiredoxin I and II. |
| in vivo study | Conoidin a (intraperitoneal injection; 5 mg/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: 5 mg/kg Administration: Intraperitoneal injection; 5 mg/kg; for three successive days before MI/R injury Result: Significantly reversed the antioxidative effect of Luteolin. Impaired the protective effects of luteolin. |
| 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. |
Last Update：2024-04-10 22:30:50
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CAS: 18080-67-6
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CAS: 18080-67-6
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Mobile: 18021002903
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