(E/Z)-Ozagrel sodium
(E/Z)-Ozagrel sodium [(E/Z)-OKY-046 sodium] is an EZ configuration mixture of Ozagrel sodium (HY-B0428A). Ozagrel sodium (OKY-046 sodium) is a high selective and orally active thromboxane A2 (TXA2) synthase inhibitor with an IC50 of 11 nM. Ozagrel sodium exerts anti-platelet aggregation, vasodilation and anti-inflammatory effects by inhibiting the production of TXA2 and increasing the production of prostacyclin (PGI2). Ozagrel sodium can be used for the study of ischemic stroke, asthma and thromboembolic diseases.
For research use only. We do not sell to patients.
- CAS No.: 130952-46-4
- Formula: C13H11N2NaO2
- Molecular Weight:250.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1][5]|
TXA2 11 nM (IC50) |
TXB2 |
Chemical Information
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CAS No. 130952-46-4
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Molecular Weight 250.23
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Formula C13H11N2NaO2
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SMILES
O=C(O[Na])/C=C/C1=CC=C(CN2C=CN=C2)C=C1
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Synonyms
(E/Z)-OKY-046 sodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
[1]. Saito MS, et al. Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization. J Enzyme Inhib Med Chem. 2016 Dec;31(6):1591-601. [Content Brief]
[2]. Bhatia P, Singh N. Ameliorative effect of ozagrel, a thromboxane A2 synthase inhibitor, in hyperhomocysteinemia-induced experimental vascular cognitive impairment and dementia. Fundam Clin Pharmacol. 2021 Aug;35(4):650-666. [Content Brief]
[3]. Bhatia P, Kaur G, Singh N. Ozagrel a thromboxane A2 synthase inhibitor extenuates endothelial dysfunction, oxidative stress and neuroinflammation in rat model of bilateral common carotid artery occlusion induced vascular dementia. Vascul Pharmacol. 2021 Apr;137:106827. [Content Brief]
[4]. Ishitsuka Y, et al. A selective thromboxane A2 (TXA2) synthase inhibitor, ozagrel, attenuates lung injury and decreases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in oleic acid-induced lung injury in guinea pigs. J Pharmacol Sci. 2009 Oct;111(2):211-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)