SC57666
目录号 : GC31960
SC57666是选择性的COX2抑制剂，IC50值为26nM。
Cas No.:158959-32-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM.
SC57666 inhibits COX2 with an IC50 of 3.2±0.8 nM in CHO cells stably transfected with human COX isozymes, with 1000 fold or more selectivity over COX1 (IC50=6000±1900 nM)[2].
SC57666 has been shown to be orally active (ED50=1.7 mpk) in the adjuvant-induced arthritis model. No gastric lesions are observed in mice after 5 h when SC57666 is administered intragastrically at 600 mpk. No intestinal damage is observed in rats after 72 h when SC57666 is administered intragastrically at 200 mpk[1].
[1]. Reitz DB, et al. Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally activeCOX2 inhibitors. J Med Chem. 1994 Nov 11;37(23):3878-81. [2]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.
| Cas No. | 158959-32-1 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(C2=C(C3=CC=C(F)C=C3)CCC2)C=C1)(C)=O | ||
| 分子式 | C18H17FO2S | 分子量 | 316.39 |
| 溶解度 | DMSO: ≥ 100 mg/mL (316.07 mM) | 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 | 3.1607 mL | 15.8033 mL | 31.6066 mL |
| 5 mM | 0.6321 mL | 3.1607 mL | 6.3213 mL |
| 10 mM | 0.3161 mL | 1.5803 mL | 3.1607 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。
In-vitro test system for the evaluation of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibitors based on a single HPLC run with UV detection using bovine aortic coronary endothelial cells (BAECs)
Objective and design: The aim of this study was to develop a new, whole-cell test system which is easy to handle and requires a standard equipment for the parallel screening of COX-1 and COX-2 inhibitors. Materials: Bovine aortic endothelial cells (BAECs). Treatment and methods: Unstimulated bovine aortic coronary endothelial cells (BAECs) were used as a source of COX-1 and BAECs pretreated with ASA (100 microM) and activated with phorbol myristate acetate (PMA) were used as a source of COX-2. The time- and concentration-dependent induction of COX-2 expression in the BAECs was evaluated by a kinetic profile (HPLC analysis) and detected by Western-Blot analysis using polyclonal antibodies against COX-1 and COX-2. Results: In BAECs, diclofenac and meloxicam showed balanced inhibition of COX-1 (IC50: 0.01/0.4 microM) and COX-2 (IC50: 0.03/0.6 microM). Indomethacin inhibited COX-1 more potently than COX-2 (IC50: 0.008/0.04 microM). Aceclofenac inhibited COX-2 more potently than COX-1 (IC50: 3.0/7.3 microM). DFU and Cl-SC57666 [16] inhibited COX-2 (IC50: 0.04/0.001 microM) highly selectively but did not inhibit COX-1 (IC50: >100 microM). Conclusions: In summary an assay has been developed, for the determination of IC50-values for inhibitors of COX-1/2 on cells of the same origin, in line with values in the literature. Moreover, new insights have been gained into the relationship of COX-1/2 and lipoxygenase pathways in BAECs by detecting 15- and 12-HETE: Inhibition of COX-1 by the NSAIDs mostly resulted in an enhancement of 15-HETE and 12-HETE release. In contrast inhibition of COX-2 decreased 15-HETE release.