Febuxostat D9
(Synonyms: 非布司他 D9) 目录号 : GC36036
An internal standard for the quantification of febuxostat
Cas No.:1246819-50-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Febuxostat-d9 is intended for use as an internal standard for the quantification of febuxostat by GC- or LC-MS. Febuxostat is an antihyperuricemic nonpurine inhibitor of both the oxidized and reduced forms of xanthine oxidase.1 It inhibits bovine milk xanthine oxidase as well as mouse and rat liver xanthine oxidase/xanthine dehydrogenase (IC50s = 1.4, 1.8, and 2.2 nM, respectively).2 It is 10-30 times more potent than the hypoxanthine analog allopurinol .3,4 Febuxostat decreases the serum level of urate in a potassium oxonate rat model of hyperuricemia (ED50 = 1.5 mg/kg).2 It reduces hepatic macrovesicular steatosis in mice fed a high-fat diet containing trans fatty acids when administered at a dose of 1 mg/kg per day.5 Febuxostat (0.75 mg/kg) also increases CNS expression of glutamate oxaloacetate transaminase 2 (GOT2) and improves neurological symptoms in a mouse model of secondary progressive experimental autoimmune encephalomyelitis (EAE).6 Formulations containing febuxostat have been used in the treatment of symptomatic hyperuricemia in patients with gout.
1.Okamoto, K., Eger, B.T., Nishino, T., et al.An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibitionJ. Biol. Chem.278(3)1848-1855(2003) 2.Osada, Y., Tsuchimoto, M., Fukushima, H., et al.Hypouricemic effect of the novel xanthine oxidase inhibitor, TEI-6720, in rodentsEur. J. Pharmacol.241(2-3)183-188(1993) 3.Takano, Y., Hase-Aoki, K., Horiuchi, H., et al.Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenaseLife Sci.76(16)1835-1847(2005) 4.Bisht, M., and Bist, S.S.Febuxostat: A novel agent for management of hyperuricemia in goutIndian J. Pharm. Sci.73(6)597-600(2011) 5.Nakatsu, Y., Seno, Y., Kushiyama, A., et al.The xanthine oxidase inhibitor febuxostat suppresses development of nonalcoholic steatohepatitis in a rodent modelAm. J. Physiol. Gastrointest. Liver Physiol.309(1)G42-G51(2015) 6.Honorat, J.A., Nakatsuji, Y., Shimizu, M., et al.Febuxostat ameliorates secondary progressive experimental autoimmune encephalomyelitis by restoring mitochondrial energy production in a GOT2-dependent mannerPLoS One12(11)e0187215(2017)
| Cas No. | 1246819-50-0 | SDF | |
| 别名 | 非布司他 D9 | ||
| Canonical SMILES | CC1=C(C(O)=O)SC(C2=CC=C(OC([2H])([2H])C(C([2H])([2H])[2H])([2H])C([2H])([2H])[2H])C(C#N)=C2)=N1 | ||
| 分子式 | C16H7D9N2O3S | 分子量 | 325.43 |
| 溶解度 | DMSO: 1 mg/ml | 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 | 3.0729 mL | 15.3643 mL | 30.7286 mL |
| 5 mM | 0.6146 mL | 3.0729 mL | 6.1457 mL |
| 10 mM | 0.3073 mL | 1.5364 mL | 3.0729 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。