Furegrelate (sodium salt)
(Synonyms: U-63557A) 目录号 : GC13536
A potent inhibitor of thromboxane synthase
Cas No.:85666-17-7
Sample solution is provided at 25 µL, 10mM.
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Furegrelate (sodium salt) is a potent inhibitor of thromboxane synthase [1][2].
Thromboxane A synthase 1 (platelet, cytochrome P450, family 5, subfamily A) is a cytochrome P450 enzyme that catalyzes the conversion of prostaglandin H2 to thromboxane A2. Thromboxanes play an important role in vasoconstriction and platelet aggregation.
Furegrelate (sodium salt), also known as sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate (U-63557A), is a potent, specific and orally available thromboxane synthase inhibitor. U-63557A is a potent inhibitor of the thromboxane synthase in human platelets in vitro, as well as in rhesus monkey platelets ex vivo. U-63557A didn’t inhibit thrombin-stimulated PGI2 biosynthesis in human endothelial cells, the 5-lipoxygenase in human neutrophils, or the cyclooxygenase in a variety of test systems [2].
In rhesus monkeys, U-63557A inhibited the platelet thromboxane synthase by approximately 80% for at least 12 hrs. In anesthetized dogs, U-63557A inhibited the blockage of stenosed coronary arteries caused platelet aggregation. While the protective effects of U-63557A could be reversed by cyclooxygenase inhibitors. U-63557A is a promising compound for the evaluation of the role of thromboxane synthase in a variety of pathophysiological states [2].
References:
[1]. Johnson RA, Nidy EG, Aiken JW, et al. Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids. J Med Chem. 1986 Aug;29(8):1461-8.
[2]. Gorman RR, Johnson RA, Spilman CH, et al. Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate. Prostaglandins. 1983 Aug;26(2):325-42.
| Cas No. | 85666-17-7 | SDF | |
| 别名 | U-63557A | ||
| 化学名 | 5-(3-pyridinylmethyl)-2-benzofurancarboxylic acid, sodium salt | ||
| Canonical SMILES | O=C(C1=CC2=C(O1)C=CC(CC3=CN=CC=C3)=C2)[O-].[Na+] | ||
| 分子式 | C15H10NO3 • Na | 分子量 | 275.2 |
| 溶解度 | ≤15mg/ml in Water | 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 | 3.6337 mL | 18.1686 mL | 36.3372 mL |
| 5 mM | 0.7267 mL | 3.6337 mL | 7.2674 mL |
| 10 mM | 0.3634 mL | 1.8169 mL | 3.6337 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet