1,4-二氧代-2,3-二溴甲基喹啉

生物活性靶点体外研究体内研究 1,4-二氧代-2,3-二溴甲基喹啉试剂级价格

1,4-二氧代-2,3-二溴甲基喹啉

CAS号:18080-67-6
英文名:2,3-BIS(BROMOMETHYL)QUINOXALINE 1,4-DIOXIDE
中文名:1,4-二氧代-2,3-二溴甲基喹啉
CBNumber:CB72455090
分子式:C10H8Br2N2O2
分子量:347.99
MOL File:18080-67-6.mol

1,4-二氧代-2,3-二溴甲基喹啉化学性质

熔点 :180-190 °C (decomp)
沸点 :512.3±60.0 °C(Predicted)
密度 :1.95±0.1 g/cm3(Predicted)
溶解度 :DMF: 25 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 20 mg/ml
形态 :A crystalline solid
酸度系数(pKa) :1.91±0.30(Predicted)
颜色 :White to yellow

1,4-二氧代-2,3-二溴甲基喹啉性质、用途与生产工艺

生物活性 Conoidin A 是刚地弓形虫过氧化物酶 II (TgPrxII) 的细胞通透性抑制剂，有杀线虫的特性。Conoidin A 共价结合 TgPrxII 的过氧化物催化位点 Cys47，不可逆地抑制其过氧化物活性，IC50 为 23 µM。Conoidin A 也抑制哺乳动物 PrxI 和 PrxII (但不抑制 PrxIII) 的氧化。Conoidin A 具有抗氧化、神经保护作用，并且可用于缺血性心脏病的研究。
靶点

IC50: 23 µM ( T. gondii enzyme peroxiredoxin II (TgPrxII))
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.