D01684
Ozagrel sodium
CAS: 189224-26-8;130952-46-4
Molecular Formula: C13H11N2NaO2
D01684 - Names and Identifiers
| Name | Ozagrel sodium |
| Synonyms | Ozapen D01684 Athrombone Ozapen (tn) OZAGREL SODIUM Ozagrel sodium Ozagrel sodium (jan) sodium (E)-3-(4-((1H-imidazol-1-yl)methyl)phenyl)acrylate sodium (2E)-3-[4-(1H-imidazol-1-ylmethyl)phenyl]prop-2-enoate (E)-3-[4-(1H-Imidazol-1-ylmethyl)phenyl]acrylic acid sodium salt (2E)-3-[4-(1H-Imidazol-1-ylmethyl)phenyl]-2-propenoic acid sodium salt |
| CAS | 189224-26-8 130952-46-4 |
| EINECS | 1806241-263-5 |
| InChI | InChI=1/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/b6-5+ |
D01684 - Physico-chemical Properties
| Molecular Formula | C13H11N2NaO2 |
| Molar Mass | 250.23 |
| Storage Condition | -20℃ |
D01684 - Nature
Open Data Verified Data
White Crystal or crystalline powder, odorless, sour bitter. Soluble in water, soluble in methanol, almost insoluble in ethanol, acetone or ether.
Last Update：2024-01-02 23:10:35
D01684 - Preparation Method
Open Data Verified Data
using p-methylbenzaldehyde as a raw material, the mixture was subjected to aldol condensation with acetic anhydride, followed by dehydration to obtain 3 pairs of tolylacrylic acid, which was esterified to ethyl 3-p-tolylacrylate. Sodium ozagrel was obtained by hydrolysis of N-bromosuccinimide bromination with benzoyl peroxide as initiator and reaction with imidazole.
Last Update：2022-01-01 09:23:44
D01684 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.996 ml | 19.982 ml | 39.964 ml |
| 5 mM | 0.799 ml | 3.996 ml | 7.993 ml |
| 10 mM | 0.4 ml | 1.998 ml | 3.996 ml |
| 5 mM | 0.08 ml | 0.4 ml | 0.799 ml |
Last Update：2024-01-02 23:10:35
D01684 - Use
Open Data Verified Data
developed by nipponao Pharmaceutical Industry Co., Ltd., was first launched in Japan in April 1988. Potent thromboxane synthase inhibitors. By inhibiting thromboxane synthase, lowering thromboxane A2(TXA2) in vivo, and promoting the production of prostacyclin (PGI2), to fight against the aggregation of platelets and spasm of cerebral vessels, however, it had little effect on other arachidonic acid metabolizing enzymes such as cyclooxygenase. For the improvement of vasospasm after subarachnoid hemorrhage surgery and its complicated cerebral ischemia symptoms.
Last Update：2022-01-01 09:23:44
D01684 - Safety
Open Data Verified Data
male and female mice, male and female rats LD50 (mg/kg): 1940, 1580, 1150, 1300 intravenous injection; 3800, 3600, 5900, 5700 oral; 2450, 2250, 0.
Last Update：2022-01-01 09:23:44
D01684 - Reference Information
| Thromboxane (TXA) Synthase Inhibitor | Sodium ozagrel is the sodium salt form of the antiplatelet agglutination agent ozagrel. It is a thromboxane (TXA) synthase inhibitor that can selectively inhibit thromboxane synthase and inhibit TXA synthesis, thereby inhibiting the production of TXA2 and promoting the production of prostacyclin (PGI2), it has the effect of anti-platelet aggregation and relieving vasospasm. Can inhibit cerebral embolism and cerebral vasospasm. A single intravenous injection of human blood disappeared quickly, continuous administration of 2h that is to achieve steady-state blood drug concentration, stop administration of 24h after most of the row. Figure 1 is the structural formula of sodium ozagrel. |
| pharmacological action | sodium ozagrel is a thromboxane synthase inhibitor, which can inhibit TXA2 production, so it has anti-platelet accumulation and vasodilation effects. Animal experiments showed that intravenous administration could reduce plasma TXB2 level, decrease Keto-PGF12/TXB2 ratio, inhibit platelet aggregation caused by different inducers, and prevent cerebral infarction caused by middle cerebral artery in rats. |
| pharmacokinetics | after intravenous drip of this product, the blood concentration-time curve conforms to the two-compartment open model, T1/2β is 1.22±0.44h,Vd is 2.32±0.62l/kg,AUC is 0.47±0.08 μ g hr/nl. Cl is 3.25±0.82l/h/kg, the longest half-life of the subject is 1.93h, and the blood drug concentration can be measured to 3h after drug withdrawal. After stopping the drug for 24 hours, almost all the drugs were excreted in urine. |
| indication | is suitable for the treatment of acute thrombotic cerebral infarction, vasospasm after subarachnoid hemorrhage and the improvement of cerebral ischemia symptoms. |
| usage and dosage | to improve cerebral thrombosis (acute phase):40~80mg, dissolve with appropriate amount of electrolyte or GS, and continue to drip for 2 hours, bid for 1~2 weeks. To improve cerebral vasospasm and cerebral ischemia symptoms after subarachnoid hemorrhage surgery: 80mg,qd,24 hours continuous intravenous drip for 2 weeks. The dose can be appropriately increased or decreased according to age and symptoms. |
| adverse reactions | blood: bleeding tendency may occur, if there is abnormal bleeding, stop administration. Liver and kidney: Occasionally increased GOT, GPT and BUN. Digestive system: occasional belching, loss of appetite, vomiting, and increased aminotransferase. Rashes are occasional and should be discontinued. Anaphylaxis: Occasionally urticaria, rash, etc., stop administration when it occurs. Circulatory system: occasionally supraventricular premature contraction, blood pressure drop, when found to reduce the dose or stop the administration. Other: Occasional symptoms such as headache, fever, pain at the injection site, shock and thrombocytopenia. Severe adverse reactions can be hemorrhagic cerebral infarction, epidural hematoma, intracerebral hemorrhage, gastrointestinal hemorrhage, subcutaneous hemorrhage, etc. |
| drug interaction | 1. ozagrel sodium injection combined with antiplatelet aggregation agents, thrombolytic agents and other anticoagulants can enhance bleeding tendency and must be appropriately reduced. 2. Avoid mixing this product with calcium infusion (Green's solution, etc.) to avoid white turbidity. 3. Use with caution for pregnant women or women who may become pregnant. |
| precautions | 1, some hemorrhagic diseases (such as hemorrhagic cerebral infarction, epidural hemorrhage, intracranial hemorrhage, intraventricular hemorrhage) are prohibited. 2. Those with a history of allergy to this product are prohibited. 3. Patients with bleeding tendency, history of gastrointestinal hemorrhage, severe hypertension, severe diabetes, and thrombocytopenia should be used with caution. 4. Caution should be taken when combined with other antiplatelet drugs, thrombolytic drugs and anticoagulants. |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: Ozagrel Sodium Salt Visit Supplier Webpage Request for quotationCAS: 189224-26-8
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Ozagrel sodium Visit Supplier Webpage Request for quotationCAS: 130952-46-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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