T52231 |
Conoidin A |
MedMol | 98% |
- 产品描述: Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease
- 靶点: Toxoplasma
- 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 activity in vitro. Conoidin A also shown to alkylate or crosslink catalytic cysteines of wild type AcePrx-1 in Ancylostoma ceylanicum and 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; 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.
- 参考文献:
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
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
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 50 mM 0.057 ml 0.287 ml 0.575 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)