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Ozagrel

Catalog No. T6236   CAS 82571-53-7
Synonyms: OKY-046, Domenan

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

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Ozagrel Chemical Structure
Ozagrel, CAS 82571-53-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 52.00
25 mg In stock $ 86.00
50 mg In stock $ 121.00
100 mg In stock $ 182.00
200 mg In stock $ 236.00
500 mg In stock $ 396.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 100%
Purity: 99.55%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
Targets&IC50 TXA2 synthase:11 nM
In vivo Ozagrel (3 mg/kg) decreases both the area and volume of the cortical infarction after ischemia-reperfusion of the middle cerebral artery in rat. Ozagrel also has suppressive effects on the neurologic deficits in the microthrombosis rat model. Ozagrel improves the reduced spontaneously locomotor activity and the obstruction of motor coordination in the conscious cerebral ischemia-reperfusion mouse model. Ozagrel prevents oleic acid (OA)-induced thromboxane A(2) generation and subsequently increased total protein concentration and the numbers of macrophages and neutrophils in bronchoalveolar lavage fluid and increases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in the whole lung of guinea pigs. Ozagrel suppresses the decrease in specific gravity of the brain tissue induced by the occlusion-reperfusion in the conscious cerebral ischemia-reperfusion SHR model, and recovers the postischemic decrease in cortical PO(2) after middle cerebral artery occlusion-reperfusion in cats. Ozagrel administered intravenously 30 min before oleic acid injection prevents the decrease in Pao(2) and pulmonary vascular hyper-permeability in guinea-pigs. Ozagrel also prevents increases in lactate dehydrogenase activity, a measure of lung cell injury, TXB(2) and its weight ratio to 6-keto prostaglandin F(1alpha) in bronchoalveolar lavage fluid in guinea-pigs. Ozagrel also increases the level of 6-keto-PGF(1alpha), a metabolite of prostaglandin I(2) (PGI(2)), in the brain tissue after cerebral ischemia-reperfusion, and the administration of PGI(2) improves the reduced spontaneous locomotor activity in the conscious cerebral ischemia-reperfusion mouse model.
Kinase Assay In vitro kinase assays: The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.
Synonyms OKY-046, Domenan
Molecular Weight 228.25
Formula C13H12N2O2
CAS No. 82571-53-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 43 mg/mL (188.4 mM)

TargetMolReferences and Literature

1. Ishitsuka Y, et al. J Pharmacol Sci, 2009, 111(2), 211-215. 2. Imamura T, et al. Arzneimittelforschung, 2003, 53(10), 688-694. 3. Ichikawa K, et al. Pharmacology, 1999, 59(5), 257-265. 4. Ishitsuka Y, et al. J Pharm Pharmacol, 2004, 56(4), 513-520. 5. Naito J, et al. Eur J Pharmacol. 1983, 91(1), 41-48.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library GPCR Compound Library Coagulation and Anticoagulation Compound Library Bioactive Compounds Library Max Protease Inhibitor Library Drug-Fragment Library

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Keywords

Ozagrel 82571-53-7 GPCR/G Protein Immunology/Inflammation Proteases/Proteasome Prostaglandin Receptor Thrombin TXA2 aggregation OKY046 OKY-046 Inhibitor Domenan OKY 046 thromboxane A2 antiplatelet inhibit platelet inhibitor

 

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