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18080-67-6

中文名稱 1,4-二氧代-2,3-二溴甲基喹啉
英文名稱 2,3-BIS(BROMOMETHYL)QUINOXALINE 1,4-DIOXIDE
CAS 18080-67-6
分子式 C10H8Br2N2O2
分子量 347.99
MOL 文件 18080-67-6.mol
更新日期 2024/12/17 09:24:26
18080-67-6 結(jié)構(gòu)式 18080-67-6 結(jié)構(gòu)式

基本信息

中文別名
1,4-二氧代-2,3-二溴甲基喹啉
英文別名
Conoidin A
2,3-BIS(BROMOMETHYL)QUINOXALINE 1,4-DIOXIDE
Quinoxaline, 2,3-bis(bromomethyl)-, 1,4-dioxide
2,3-bis(broMoMethyl)-1-oxoquinoxalin-1-iuM-4(1H)-olate
所屬類別
醫(yī)藥中間體:喹啉類化合物

物理化學性質(zhì)

熔點180-190 °C (decomp)
沸點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
酸度系數(shù)(pKa)1.91±0.30(Predicted)
形態(tài)A crystalline solid
顏色White to yellow

安全數(shù)據(jù)

危險性描述H413
防范說明P273-P501
1,4-二氧代-2,3-二溴甲基喹啉價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-1160901,4-二氧代-2,3-二溴甲基喹啉
Conoidin A
18080-67-625mg500元
2024/11/08HY-1160901,4-二氧代-2,3-二溴甲基喹啉
Conoidin A
18080-67-610mM * 1mLin DMSO550元
2024/11/08HY-1160901,4-二氧代-2,3-二溴甲基喹啉
Conoidin A
18080-67-6100mg1000元

常見問題列表

生物活性
Conoidin A 是剛地弓形蟲過氧化物酶 II (TgPrxII) 的細胞通透性抑制劑,有殺線蟲的特性。Conoidin A 共價結(jié)合 TgPrxII 的過氧化物催化位點 Cys47,不可逆地抑制其過氧化物活性,IC50 為 23 μM。Conoidin A 也抑制哺乳動物 PrxI 和 PrxII (但不抑制 PrxIII) 的氧化。Conoidin A 具有抗氧化、神經(jīng)保護作用,并且可用于缺血性心臟病的研究。
靶點

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

體外研究

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.

體內(nèi)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.
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