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Merck
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Key Documents

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SML3274

Sigma-Aldrich

AZD5904

≥95% (HPLC)

Sinónimos:

(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

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About This Item

Fórmula empírica (notación de Hill):
C10H12N4O2S
Número de CAS:
618913-30-7
Peso molecular:
252.29
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

O=C1NC(N(C[C@@H]2OCCC2)C3=C1NC=N3)=S

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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
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
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
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
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