SML3274
AZD5904
≥95% (HPLC)
Synonym(s):
(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
Empirical Formula (Hill Notation):
C10H12N4O2S
CAS Number:
Molecular Weight:
252.29
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
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
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.
Highly selective and orally available mechanism-based myeloperoxidase (MPO) inactivatior with in vitro and in vivo efficacy.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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
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
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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3274-5MG | 04065267044798 |
| SML3274-25MG | 04065267044781 |