SML3274
AZD5904
≥95% (HPLC)
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
质量水平
方案
≥95% (HPLC)
表单
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
InChI
1S/C10H12N4O2S/c15-9-7-8(12-5-11-7)14(10(17)13-9)4-6-2-1-3-16-6/h5-6H,1-4H2,(H,11,12)(H,13,15,17)/t6-/m1/s1
InChI key
RSPDBEVKURKEII-ZCFIWIBFSA-N
相关类别
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.
Highly selective and orally available mechanism-based myeloperoxidase (MPO) inactivatior with in vitro and in vivo efficacy.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
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
Yesica Garciafigueroa et al.
Frontiers in endocrinology, 12, 565981-565981 (2021-03-30)
A growing body of evidence indicates that neutrophils are the first major leukocyte population accumulating inside the pancreas even before the onset of a lymphocytic-driven impairment of functional beta cells in type 1 diabetes mellitus (T1D). In humans, pancreata from
Sophie L Maiocchi et al.
Biochemical pharmacology, 135, 90-115 (2017-03-28)
The leukocyte-derived heme enzyme myeloperoxidase (MPO) is released extracellularly during inflammation and impairs nitric oxide (NO) bioavailability by directly oxidizing NO or producing NO-consuming substrate radicals. Here, structurally diverse pharmacological agents with activities as MPO substrates/inhibitors or antioxidants were screened
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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