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
- 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.
- 更新日期:2024/11/08
- 产品编号:HY-116090
- 产品名称:1,4-二氧代-2,3-二溴甲基喹啉 Conoidin A
- CAS编号:18080-67-6
- 包装:25mg
- 价格:500元
- 更新日期:2024/11/08
- 产品编号:HY-116090
- 产品名称:1,4-二氧代-2,3-二溴甲基喹啉 Conoidin A
- CAS编号:18080-67-6
- 包装:10mM * 1mLin DMSO
- 价格:550元
- 公司名称:Otto Chemie Pvt. Ltd.
- 联系电话:--
- 电子邮件:info@ottokemi.com
- 国家:印度
- 产品数:5870
- 优势度:58
- 公司名称:A.J Chemicals
- 联系电话:--
- 电子邮件:sales@ajchem.in
- 国家:印度
- 产品数:6100
- 优势度:58