Ozagrel sodium
(Synonyms: 奥扎格雷钠; OKY-046 sodium) 目录号 : GC36831
A selective inhibitor of TXA synthase
Cas No.:189224-26-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Inhibition of thromboxane synthase (TXAS), especially in human platelets, has been a clinical objective for many years. 1-
1.Iizuka, K., Akahane, K., Momose, D., et al.Highly selective inhibitors of thromboxane synthase. 1. Imidazole derivativesJ. Med. Chem.241139-1148(1981) 2.Wright, W.B., Tomcufcik, A.S., Chan, P.S., et al.Thromboxane synthase inhibitors and antihypertensive agents. 4,N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-onesJ. Med. Chem.302277-2283(1987) 3.Wright, W.B., Jr., Press, J.B., Chan, P.S., et al.Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-imidazol-1,2,4-triazol-1-yl)alkyl]aryl amidesJ. Med. Chem.29523-530(1986) 4.Ichikawa, K., Tazawa, S., Hamano, S., et al.Effect of ozagrel on locomotor and motor coordination after transient cerebral ischemia in experimental animal modelsPharmacology59257-265(1999) 5.Press, J.B., Wright, W.B., Jr., Chan, P.S., et al.Thromboxane synthetase inhibitors and antihypertensive agents. 2. N-[(1H-Imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones and N-[(1H-1,2,4-triazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones as unique antihypertensive agentsJ. Med. Chem.29(5)816-819(1986)
| Cas No. | 189224-26-8 | SDF | |
| 别名 | 奥扎格雷钠; OKY-046 sodium | ||
| Canonical SMILES | O=C([O-])/C=C/C1=CC=C(CN2C=CN=C2)C=C1.[Na+] | ||
| 分子式 | C13H11N2NaO2 | 分子量 | 250.23 |
| 溶解度 | Water: ≥ 44 mg/mL (175.84 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Prediction of compatibility between Ozagrel sodium preparation for injection and calcium on the basis of the solubility product
Chem Pharm Bull (Tokyo) 2013;61(5):567-71.PMID:23449252DOI:10.1248/cpb.c13-00042.
The purpose of the study was to evaluate the compatibility of Ozagrel sodium solution and calcium-containing transfusions using solubility product constants. We calculated the solubility product constant of mixtures of Ozagrel sodium and calcium chloride and evaluated the compatibility of Ozagrel sodium solution (both the original and generic products) with calcium chloride solution using a light obscuration particle counter. Various volumes of ozagrel solution were added to the calcium solutions to make final ozagrel concentrations of 0, 0.8, 1.6, 2.0, 2.4, 3.2 and 4.0 mmol/L. The solutions were gently agitated and stored at 25 and 40°C. The ozagrel concentration, calcium ion concentration and number of microparticles were measured. The solubility product constants obtained were 11.89×10(-9) mol(3)/L(3) (at 25°C) and 7.82×10(-9) mol(3)/L(3) (40°C). The number of insoluble microparticles was significantly increased when the ionic product was larger than the solubility product constant. In all Ozagrel sodium products, the number of insoluble microparticles was within the allowable range according to the Japanese Pharmacopoeia. These results suggest that mixing Ozagrel sodium with calcium-containing products is safe and without appreciable risk of incompatibility under clinical conditions.
Ozagrel for Postoperative Management of Aneurysmal Subarachnoid Hemorrhages
Neurol India 2019 Sep-Oct;67(5):1286-1289.PMID:31744960DOI:10.4103/0028-3886.271236.
Background: A number of pharmacological agents have been tried to circumvent the problem of delayed cerebral ischemia (DCI) with Ozagrel sodium being one such agent aimed at the prevention of DCI. Ozagrel is an inhibitor of thromboxane synthetase. It has anti-platelet aggregation action and it dilates vessels. Ozagrel was not available outside Japan till recently. It is available now in India and we had the opportunity to use it among patients with aneurysmal subarachnoid hemorrhage (SAH). Aims: To analyse the results of ozagrel administration for patients with aneurysmal SAH. Settings and design: Tertiary care neurosurgical center. Materials and methods: Retrospective analysis of the outcomes of patients who received ozagrel after microsurgical cllipping of aneurysm and comparison with a control grpup who received treatment as usual. Statistical analysis: The t-test (two-tailed), Chi-square test, and Mann-Whitney U-test asymptomatic significance (two-tailed), were used respectively for continuous, categorical, and ordinal variables. The significance was determined at P = 0.05 level. Results: A total of 106 patients underwent surgical clipping of their ruptured intracranial aneurysms over a period of 22 months. Forty two (39.6%) patients received ozagrel, and 62 (60.4%) received the standard treatment. Ozagrel was started at a median of one [interquartile range (IQR) 0.75] day after the surgery, and was given for a median of five (IQR 5) days after the surgery. There was no difference in age, postictal days, World Federation Neurosurgical Society grade, Fisher grade, and the size of ruptured aneurysm in patients who received ozagrel compared to the patients who did not receive ozagrel. Of the 42 patients who received ozagrel, 30 patients (71.4%) had preoperative angiographic vasospasm which improved after the administration of ozagrel. Fifteen (35.5%) patients who received ozagrel developed delayed cerebral ischemia compared to only 11 (17.2%) patients who did not receive ozagrel. Thirty-six (85.7%) patients who received ozagrel had favorable outcome at discharge compared to 52 (81.3%) patients who did not receive ozagrel. No adverse event was observed with ozagrel therapy. At 3-month follow-up, 37 patients (88.1%) who received ozagrel had favorable outcomes against 53 patients (82.8%) who did not receive ozagrel. Conclusion: Ozagrel may be a useful drug in the armamentarium to treat vasospasm after aneurysmal SAH. A future multicenter large cohort study may validate the findings of our study.
Ozagrel for Patients With Noncardioembolic Ischemic Stroke: A Propensity Score-Matched Analysis
J Stroke Cerebrovasc Dis 2016 Dec;25(12):2828-2837.PMID:27567296DOI:10.1016/j.jstrokecerebrovasdis.2016.07.044.
Background and purpose: Ozagrel sodium (ozagrel), a thromboxane A2 synthesis inhibitor, is used for ischemic stroke patients in several countries, despite a lack of strict evidence of its benefits. We investigated whether ozagrel was beneficial for patients with atherothrombotic stroke or lacunar infarction. Methods: This was a retrospective observational study using the Diagnosis Procedure Combination database in Japan. We identified patients with atherothrombotic stroke or lacunar infarction who were admitted to 781 hospitals from July 1, 2010 to March 31, 2012. Propensity score-matched analyses were performed separately for patients with atherothrombotic stroke and those with lacunar infarction, which balanced differences in baseline characteristics between patients who received ozagrel (ozagrel group) and those who did not (control group) in each stroke subtype. The modified Rankin Scale scores at discharge and occurrence of hemorrhagic complications after admission were compared between the ozagrel and control groups. Results: After the propensity score matching, 2726 pairs of patients with atherothrombotic stroke and 1612 pairs of patients with lacunar infarction were analyzed. Ordinal logistic regression analyses showed that ozagrel use was not significantly associated with modified Rankin Scale score at discharge in patients with atherothrombotic stroke (odds ratio: .99; 95% confidence interval: .88-1.11) or in those with lacunar infarction (odds ratio: 1.00; 95% confidence interval: .87-1.16). The occurrence of hemorrhagic complications did not differ significantly between the ozagrel and control groups. Conclusion: The present study suggested that ozagrel was safe to use but did not improve functional outcomes in patients with atherothrombotic or lacunar infarction.
The effect of Ozagrel sodium on photochemical thrombosis in rat: therapeutic window and combined therapy with heparin sodium
Life Sci 2002 Nov 8;71(25):2983-94.PMID:12384182DOI:10.1016/s0024-3205(02)02165-3.
The therapeutic efficacy of Ozagrel sodium (ozagrel), alone and in combination with heparin, and its therapeutic time window were studied in a photochemically induced thrombotic cerebral infarction rat model. Cerebral artery thrombosis was induced by irradiating the brain with green light through intact skull using rose bengal as the photosensitizing dye. One set of animals was treated immediately after thrombosis with (1) vehicle, (2) 10 mg/kg ozagrel in saline, intravenously (i.v.), (3) 150 U/kg unfractioned heparin, subcutaneously (s.c.), or (4) ozagrel, i.v. plus heparin, s.c. Infarct volume was significantly smaller and edema was reduced in the ozagrel-treated groups compared to the vehicle-treated group; heparin did not convey additional benefit. In another set of animals, rats were given either vehicle or 10 mg/kg ozagrel in saline, i.v., 60 min or 120 min after induction of thrombosis. Ozagrel reduced infarct volume, but its effect diminished with delayed administration. The therapeutic window was determined to be less than 60 minutes after induction of thrombosis.
[Effects of sodium ozagrel in primary thrombocytosis combined with thrombosis]
Zhongguo Shi Yan Xue Ye Xue Za Zhi 2009 Oct;17(5):1360-2.PMID:19840484doi
This study was aimed to investigate the incidence of thrombosis in patients with primary thrombocytosis (PT) and its correlation with function changes of platelets, and to explore the effect of thromboxane A2 (TXA2) inhibitor-ozagrel sodium on platelet activity and its efficacy for prevention and treatment of thrombosis. The CD62P and PAC-1 levels on platelet surface were detected by flow cytometry; the levels of TXB2 (metabolic product of TXA2) and 6-keto-PGFIalpha (metabolic product of prostacyclin) were detected by FLISA. The function change of platelets and its correlation with thrombosis were observed and compared in PT patients with and without thrombosis. The results indicated that the TXB2, PAC-1 and CD62P level, and TXB2/6-keto-PGF1alpha ratio in PT patients with thrombosis were higher than those in PT patients without thrombosis before treatment with Ozagrel sodium (p<0.01). After treatment with Ozagrel sodium, the function indexes of platelets such as CD62P, PAC-1, TXB2 and TXB2/6-keto-PGF1alpha except 6-keto-PGF1alpha in PT patients with and without thrombosis decreased obviously (p<0.01), but there was no significant difference in TXB2, 6-keto-PGF1alpha and TXB2/6-keto-PGF1alpha levels between PT patients with and without thrombosis except CD62P and PAC-1. It is concluded that the multi-index of platelets in PT patients with thrombosis are higher than that in PT patients without thrombosis, the activation of platelet function is a high risk factor for thrombosis of PT patients. The Ozagrel sodium can obviously reduce the platelet activation, decrease the production of TXA2 and ameliorate the TXB2/6-keto-PGF1alpha ratio. The Ozagrel sodium not only possesses therapeutic effect, but also preventive efficacy for thrombosis.