| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| 1g | |||
| 2g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
TXA2
Thromboxane A2 (TXA2) synthetase. |
|---|---|
| ln Vitro |
Ozagrel raised 6-keto-PGF1 alpha, one of PGI2's stable metabolites, in a variety of isolated cells and tissues, possibly through PG endoperoxides that accumulated as a result of TXA2 synthase inhibition.
Ozagrel sodium is a selective TXA2 synthetase inhibitor. It blocks platelet aggregation and reduces bronchial muscle hypersensitivity. By restricting the generation of TXA2 while facilitating the generation of prostacyclin, ozagrel sodium reduces hyperperfusion and cerebral edema. Specific IC50 values for TXA2 synthetase inhibition are available in the pharmacological literature. The compound has been used as a therapeutic agent for ischemic heart diseases, thromboembolic disorders, cerebral circulatory disorders, and asthma. |
| ln Vivo |
Ozagrel inhibits the production of thromboxane A(2) induced by oleic acid (OA), which in turn raises the total protein concentration, neutrophil and macrophage counts in bronchoalveolar lavage fluid, and increases the expression of interleukin-8 mRNA and monocyte chemoattractant protein-1 in the guinea pigs' entire lung. Ozagrel (3 mg/kg) reduces the cortical infarction's area and volume in rats following ischemia-reperfusion of the middle cerebral artery. Additionally, obagrel suppresses the neurologic deficits in the rat model of microthrombosis. In the conscious cerebral ischemia-reperfusion mouse model, omeprazole ameliorates the reduced spontaneous locomotor activity and the blockage of motor coordination. Ozagrel recovers the postischemic decrease in cortical PO(2) following middle cerebral artery occlusion-reperfusion in cats and suppresses the decrease in specific gravity of the brain tissue caused by the occlusion-reperfusion in the conscious cerebral ischemia-reperfusion SHR model. Along with improving the reduced spontaneous locomotor activity in the conscious cerebral ischemia-reperfusion mouse model, oxagrel also raises the level of 6-keto-PGF(1alpha), a metabolite of prostaglandin I(2) (PGI(2)), in the brain tissue following cerebral ischemia-reperfusion. In intravenous oxagrel-treated guinea pigs, the decrease in Pao(2) and pulmonary vascular hyper-permeability are prevented 30 minutes prior to oleic acid injection. Additionally, oxagrel prevents increases in the weight ratio of TXB(2) to 6-keto prostaglandin F(1alpha) in guinea pig bronchoalveolar lavage fluid, which is a measure of lung cell injury.
In vivo, ozagrel sodium has been used as a therapeutic agent for ischemic heart diseases, thromboembolic disorders, cerebral circulatory disorders, and asthma. It reduces hyperperfusion and cerebral edema by restricting the generation of TXA2 while facilitating the generation of prostacyclin. The compound blocks platelet aggregation and reduces bronchial muscle hypersensitivity. Specific dosing regimens and detailed efficacy data are available from clinical pharmacology studies and clinical practice. |
| Enzyme Assay |
TXA2 synthetase activity is assessed using in vitro enzyme assays with TXA2 synthetase enzyme and a substrate (e.g., prostaglandin H2). The production of TXA2 is measured by immunoassay (e.g., ELISA for TXB2, the stable metabolite of TXA2). Inhibition of TXA2 production is measured in the presence of varying concentrations of ozagrel sodium. IC50 values are calculated from dose-response curves. Platelet aggregation is assessed using platelet-rich plasma (PRP) and aggregation inducers (e.g., collagen, ADP, arachidonic acid).
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| Cell Assay |
Cellular activity is evaluated in platelets or other TXA2-producing cells. Platelets are treated with ozagrel sodium at various concentrations (typically 0.01-100 µM) and stimulated with platelet aggregation inducers. Platelet aggregation is measured using light transmission aggregometry or impedance aggregometry. TXA2 production is measured by ELISA for TXB2. The effect on prostacyclin production may be assessed in endothelial cells.
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| Animal Protocol |
Guinea pigs
In vivo efficacy is studied in animal models of cerebral ischemia, myocardial ischemia, thrombosis, and asthma. Ozagrel sodium is administered via various routes (oral, intravenous) at doses determined from pharmacokinetic and tolerability studies. Infarct size is measured in ischemia models. Platelet aggregation is assessed ex vivo. Bronchial hyperresponsiveness is assessed in asthma models. In clinical studies, ozagrel sodium has been used as a therapeutic agent for ischemic heart diseases, thromboembolic disorders, cerebral circulatory disorders, and asthma. |
| ADME/Pharmacokinetics |
Ozagrel sodium has a molecular formula of C13H11N2NaO2 and a molecular weight of 250.23 g/mol. CAS Number: 189224-26-8. Appearance: White to light yellow powder to crystal. Purity: >98.0% (T)(HPLC). The compound is soluble in methanol and insoluble in ethanol. Storage: Room temperature (recommended in a cool and dark place, <15°C); store under inert gas, air sensitive. It is a sodium salt.
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| Toxicity/Toxicokinetics |
Safety data for ozagrel sodium are well-established from clinical use. As a TXA2 synthetase inhibitor, it may have antiplatelet effects, increasing the risk of bleeding. Common adverse events may include gastrointestinal symptoms, bleeding, and allergic reactions. Hazard Statements: H371: May cause damage to organs. Precautionary Statements: P260: Do not breathe dust; P270: Do not eat, drink or smoke when using this product; P308 + P311: IF exposed or concerned: Call a POISON CENTER/doctor. The compound is for research use only and for prescription use.
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| References | |
| Additional Infomation |
Ozagrel sodium is an approved therapeutic agent used clinically for the treatment of ischemic heart diseases, thromboembolic disorders, cerebral circulatory disorders, and asthma. It is a selective TXA2 synthetase inhibitor that blocks platelet aggregation and reduces bronchial muscle hypersensitivity. Ozagrel sodium has been used in research to study the role of thromboxane A2 in cardiovascular diseases, cerebrovascular diseases, and asthma. Its mechanism of action involves the inhibition of TXA2 synthesis and the shift towards prostacyclin production, providing a balanced approach to managing conditions involving vasoconstriction and thrombosis.
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| Molecular Formula |
C13H11N2NAO2
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|---|---|
| Molecular Weight |
250.2328
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| Exact Mass |
250.071
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| Elemental Analysis |
C, 62.40; H, 4.43; N, 11.20; Na, 9.19; O, 12.79
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| CAS # |
189224-26-8
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| Related CAS # |
Ozagrel; 82571-53-7; Ozagrel hydrochloride; 78712-43-3
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| PubChem CID |
23663942
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| Appearance |
White to off-white solid powder
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| Boiling Point |
468ºC at 760 mmHg
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| Flash Point |
236.8ºC
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| LogP |
0.694
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
289
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C([O-])/C=C/C1=CC=C(CN2C=CN=C2)C=C1.[Na+]
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| InChi Key |
NCNYJCOBUTXCBR-IPZCTEOASA-M
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| InChi Code |
InChI=1S/C13H12N2O2.Na/c16-13(17)6-5-11-1-3-12(4-2-11)9-15-8-7-14-10-15;/h1-8,10H,9H2,(H,16,17);/q;+1/p-1/b6-5+;
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| Chemical Name |
sodium;(E)-3-[4-(imidazol-1-ylmethyl)phenyl]prop-2-enoate
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| Synonyms |
Ozagrel Sodium; KCT-0809; KCT 0809; KCT0809; Cataclot Xanbo
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~50 mg/mL (~199.8 mM)
DMSO: 1~6.3 mg/mL (4~25 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (2.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.62 mg/mL (2.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 70 mg/mL (279.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9963 mL | 19.9816 mL | 39.9632 mL | |
| 5 mM | 0.7993 mL | 3.9963 mL | 7.9926 mL | |
| 10 mM | 0.3996 mL | 1.9982 mL | 3.9963 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00200356 | Completed | Drug: Edaravone Drug: Sodium Ozagrel |
Cerebral Infarction | Mitsubishi Tanabe Pharma Corporation |
August 2004 | Phase 4 |
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