FR-188582
目录号 : GC33893
FR-188582是高选择性的环氧合酶(COX-2)抑制剂，IC50值为17nM。
Cas No.:189699-82-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | Human recombinant COX-1 and COX-2 are expressed in Chinese hamster ovary cells. The appropriate COX enzyme (1 μg for COX-1 and/or 3 μg for COX-2) is preincubated in 100 mM Tris-HCl buffer (pH 7.3) containing hematin (2 μM) and tryptophan (5 mM) with drugs (0.0001-100 μM) dissolved in 1% DMSO for 5 min at 37°C prior to the addition of Arachidonic acid (10 μM) for 5 min at 37°C. Reactions are terminated by the addition of 1N HCl, and PGE2 production is measured by radioimmunoassay[1]. |
Animal experiment: | Rats[1] Female Lewis rats (140-180g) at the age of 8 weeks are used. Adjuvant arthritis is induced in female Lewis rats by intradermal injection into the plantar suface of the right hind paw of 0.5 mg of a suspension of heat-killed and dried Mycobacterium tuberculosis H37 RA in 0.05 mL of liquid Paraffin (day 0). The drugs, suspended and diluted on 0.5% methylcellulose, are given orally once a day therapeutically from day 15 to day 24 after adjuvant injection. Paw volume is measured before and 15,18,21,24 days after adjuvant injection with the Volume Meter TK-105, and edema is expressed as the increase in paw volume after adjuvant injection relative to the pre-injection value for each animal.The anti-inflammatory effect is expressed as the difference in paw edema compared with that of vehicle-treated adjuvant-control rats. |
References: [1]. Ochi T, et al. The anti-inflammatory effect of FR188582, a highly selective inhibitor of cyclooxygenase-2, with an ulcerogenic sparing effect in rats. Jpn J Pharmacol. 2001 Feb;85(2):175-82. | |
FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.
In a recombinant human cyclooxygenase (COX) enzyme activity, FR-188582 (FR188582) inhibits COX-2 with an IC50 value of 17 nM, and the inhibition of prostaglandin (PG) E2 formation by FR188582 isover 6000 times more selective for COX-2 than COX-1[1].
Oral administration of FR-188582 (0.01-3.2 mg/kg) reverses paw edema in adjuvant arthritic rats and shows a therapeutic effect in a dose-dependent manner with ED50 values (95% C.L.) of 0.074 (0.00021-0.53) and 0.063 (0.0039-0.31) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively. The anti-inflammatory effect of FR-188582 (FR188582) is threefold more potent than that of Indomethacin with ED50 values (95% C.L.) of 0.24 (0.047-1.8) and 0.20 (0.021-0.79) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively[1].
[1]. Ochi T, et al. The anti-inflammatory effect of FR188582, a highly selective inhibitor of cyclooxygenase-2, with an ulcerogenic sparing effect in rats. Jpn J Pharmacol. 2001 Feb;85(2):175-82.
| Cas No. | 189699-82-9 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(C2=CC(Cl)=NN2C3=CC=CC=C3)C=C1)(C)=O | ||
| 分子式 | C16H13ClN2O2S | 分子量 | 332.8 |
| 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 | 3.0048 mL | 15.024 mL | 30.0481 mL |
| 5 mM | 0.601 mL | 3.0048 mL | 6.0096 mL |
| 10 mM | 0.3005 mL | 1.5024 mL | 3.0048 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。