Flosulide (ZK 38997)
(Synonyms: 氟舒胺,ZK 38997; CGP 28238) 目录号 : GC31818
Flosulide (ZK 38997) 是一种有效的选择性 COX-2 抑制剂，用于治疗炎症性疾病。
Cas No.:80937-31-1
Sample solution is provided at 25 µL, 10mM.
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Flosulide is a potent and selective COX-2 inhibitor, used for the treatment for inflammatory diseases.
Flosulide (1 nM-100 μM) causes a concentration-dependent and finally complete inhibition of PGE2 production in the OSC-2 cell line, but with no effect on PG formation in the OSC-1 cells. Flosulide completely suppresses mitotic activity of OSC-2 cells, whereas mitotic activity of OSC-1 cells remain unchanged[2].
In normovolemic rats, flosulide increases renal plasma flow (RPF) and and glomerular filtration rate (GFR). In hypovolemic rats, flosulide (5-25 mg/kg) reduces RPF and GFR. Flosulide at 5 mg/kg reduces 6-keto-PGF1alpha whereas at 25 mg/kg and after indomethacin at 10 mg/kg a fall in 6-keto-PGF1alpha and TXB2 appeares[1]. Flosulide (0.75 mg/day) significantly reduces proteinuria as compared to aspirin treatment. Plasma protein and albumin levels are significantly lower in the aspirin-treated group than in flosulide-treated rats[3].
[1]. Turull A, et al. Acute effects of the anti-inflammatory cyclooxygenase-2 selective inhibitor, flosulide, on renal plasma flow and glomerular filtration rate in rats. Inflammation. 2001 Apr;25(2):119-28. [2]. Zimmermann KC, et al. Cyclooxygenase-2 expression in human esophageal carcinoma. Cancer Res. 1999 Jan 1;59(1):198-204. [3]. Heise G, et al. Different actions of the cyclooxygenase 2 selective inhibitor flosulide in rats with passive Heymann nephritis. Nephron. 1998 Oct;80(2):220-6.
Cell experiment: | The proliferation of the esophageal tumor cell lines is determined using the cell proliferation kit II. Tumor cells are incubated with flosulide and NS-398 at different concentrations for 48 h in DMEM containing FCS (10%), penicillin (100 units/mL), and streptomycin (0.1 mg/mL). After this time, the XTT labeling mixture is added, followed by 4 h of incubation and measurement of absorbance at 490 nm. |
References: [1]. Turull A, et al. Acute effects of the anti-inflammatory cyclooxygenase-2 selective inhibitor, flosulide, on renal plasma flow and glomerular filtration rate in rats. Inflammation. 2001 Apr;25(2):119-28. | |
| Cas No. | 80937-31-1 | SDF | |
| 别名 | 氟舒胺,ZK 38997; CGP 28238 | ||
| Canonical SMILES | CS(=O)(NC1=CC2=C(C(CC2)=O)C=C1OC3=CC=C(F)C=C3F)=O | ||
| 分子式 | C16H13F2NO4S | 分子量 | 353.34 |
| 溶解度 | Soluble in DMSO | 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 | 2.8301 mL | 14.1507 mL | 28.3014 mL |
| 5 mM | 0.566 mL | 2.8301 mL | 5.6603 mL |
| 10 mM | 0.283 mL | 1.4151 mL | 2.8301 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet