Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ozagrel (Domenan) 是血栓烷 A2(TXA2) 合酶抑制剂,可抑制哮喘。它也是一种抗血小板剂,可选择性抑制人血小板聚集,IC50为 53.12 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 493 | 现货 | ||
25 mg | ¥ 818 | 现货 | ||
50 mg | ¥ 1,180 | 现货 | ||
100 mg | ¥ 1,810 | 现货 | ||
200 mg | ¥ 2,690 | 现货 | ||
500 mg | ¥ 4,460 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 478 | 现货 |
产品描述 | 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. |
靶点活性 | Thromboxane A2 synthetase:11 nM |
体内活性 | 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. |
激酶实验 | 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. |
别名 | 奥扎格雷, OKY-046, Domenan |
分子量 | 228.25 |
分子式 | C13H12N2O2 |
CAS No. | 82571-53-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 43 mg/mL (188.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.3812 mL | 21.9058 mL | 43.8116 mL | 109.529 mL |
5 mM | 0.8762 mL | 4.3812 mL | 8.7623 mL | 21.9058 mL | |
10 mM | 0.4381 mL | 2.1906 mL | 4.3812 mL | 10.9529 mL | |
20 mM | 0.2191 mL | 1.0953 mL | 2.1906 mL | 5.4765 mL | |
50 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1906 mL | |
100 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ozagrel 82571-53-7 GPCR/G Protein Immunology/Inflammation Proteases/Proteasome Thrombin Prostaglandin Receptor TXA2 aggregation 奥扎格雷 OKY046 OKY-046 Inhibitor Domenan OKY 046 thromboxane A2 antiplatelet inhibit platelet inhibitor