推荐产品
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
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
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
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.
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
Halla Björnsdottir et al.
Free radical biology & medicine, 89, 1024-1035 (2015-10-16)
Neutrophil extracellular traps (NETs) are mesh-like DNA fibers clad with intracellular proteins that are cast out from neutrophils in response to certain stimuli. The process is thought to depend on reactive oxygen species (ROS) generated by the phagocyte NADPH-oxidase and
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