所有图片(1)
别名:
(R)-3-(2-Tetrahydrofuryl-methyl)-2-thioxanthine, (R)-TX3, 3-[[(2R)-Tetrahydrofuran-2-yl]methyl]-2-thioxo-7H-purin-6-one, AZD 5904, AZD-5904, TX3 R-enantiomer, TX4
经验公式（希尔记法）:
C10H12N4O2S
推荐产品
质量水平
检测方案
≥95% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
O=C1NC(N(C[C@@H]2OCCC2)C3=C1NC=N3)=S
生化/生理作用
AZD5904 (TX4) is an orally active 2-thioxanthine class suicide substrate that targets myeloperoxidase (MPO) for mechanism-based inactivation, covalently modifying MPO heme group without converting the enzyme to compound II. AZD5904 effectively inhibits peroxide-induced human MPO chlorination activity (IC50 = 0.2 μM) and extracellular MPO activity in PMA-stimulated human neutrophil cultures (by 68% at 1 μM). Oral administration (20-180 μmol/kg) of the racemate (TX3) is efficacious in reducing inflammation site MPO activity in mice in vivo with 10- to 19-fold selectivity over lactoperoxidase (LPO), thyroid peroxidase (TPO), and >70-fold selectivity over a panel of other enzymes, ion channels, and receptors.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Chrishan J A Ramachandra et al.
Cardiovascular research, 118(2), 517-530 (2021-03-12)
Hypertrophic cardiomyopathy (HCM) is characterized by cardiomyocyte hypertrophy and disarray, and myocardial stiffness due to interstitial fibrosis, which result in impaired left ventricular filling and diastolic dysfunction. The latter manifests as exercise intolerance, angina, and dyspnoea. There is currently no
Weidong Chai et al.
American journal of physiology. Endocrinology and metabolism, 317(6), E1063-E1069 (2019-10-09)
A high-fat diet (HFD) can rapidly recruit neutrophils to insulin target tissues and within days induce microvascular insulin resistance (IR). Myeloperoxidase (MPO) is highly enriched in neutrophils, can inhibit nitric oxide-mediated vasorelaxation in vitro and is associated with increased cardiovascular
Lars B Nilsson et al.
Rapid communications in mass spectrometry : RCM, 26(12), 1399-1406 (2012-05-18)
The investigations in this article were triggered by two observations in the laboratory; for some liquid chromatography/tandem mass spectrometry (LC/MS/MS) systems it was possible to obtain linear calibration curves for extreme concentration ranges and for some systems seemingly linear calibration
Reena J Popat et al.
JCI insight, 2(2), e87379-e87379 (2017-02-01)
Anti-neutrophil cytoplasmic antibody (ANCA) vasculitis is characterized by the presence of autoantibodies to myeloperoxidase and proteinase-3, which bind monocytes in addition to neutrophils. While a pathological effect on neutrophils is acknowledged, the impact of ANCA on monocyte function is less
Anna-Karin Tidén et al.
The Journal of biological chemistry, 286(43), 37578-37589 (2011-09-02)
Myeloperoxidase (MPO) is a prime candidate for promoting oxidative stress during inflammation. This abundant enzyme of neutrophils uses hydrogen peroxide to oxidize chloride to highly reactive and toxic chlorine bleach. We have identified 2-thioxanthines as potent mechanism-based inactivators of MPO.
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