SC-236 是具有口服活性的COX-2特异性抑制剂 (对 COX-1 的IC50值为 10 nM)和PPARγ激动剂。SC-236 可通过 c-Jun 氨基端抑制激活蛋白-1 (AP-1) 活性。SC-236在小鼠模型中通过抑制 ERK 的磷酸化发挥抗炎作用。
| 生物活性 | SC-236 is an orally activeCOX-2specific inhibitor (IC50= 10 nM) and aPPARγagonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation ofERKin a murine model[1][2][3][4][5]. |
| IC50& Target[5] | COX-2 10 nM (IC50) | COX-1 17.8 μM (IC50) |
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体外研究
(In Vitro) | SC-236 (15 μM, 30 min) suppresses the side effects of NSAIDs and prevented inflammation in vECs subjected to ALSS[1].
SC-236 significantly induces PPARγ expression in HSCs and acted as a potent PPARγ agonist in a luciferase-reporter trans-activation assay[2].
SC-236 strongly inhibits, in a time- and concentration-dependent manner, macrophage
viability[2].
SC-236, either alone or in combination with 15d-PGJ2, induced a marked pro-apoptotic effect in HSCs in culture[2].
SC-236 mediates antitumor effect by modulation of AP-1-signaling pathway[3].
Western Blot Analysis[1] | Cell Line: | vECs. | | Concentration: | 15 μM | | Incubation Time: | 30 min. | | Result: | Showd significant reduction in COX-2 level and increase in IκBα level, thus preventing ALSS-induced NFκB activation and inflammation in vECs. |
Western Blot Analysis[2] | Cell Line: | COS 7 cells. | | Concentration: | 3 and 10 μM. | | Incubation Time: | 18 h (combined with 15d-PGJ2). | | Result: | Acted in a concentration-dependent manner as a PPARγ agonist. |
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体内研究
(In Vivo) | SC-236 (6 mg/kg, gavage) exhibits anti-fibrotic properties in CCl4- treated animals[2].
| Animal Model: | Seventy-six male adult Wistar rats weighing 200-220 g (CCl4-treated)[2]. | | Dosage: | 6 mg/kg. | | Administration: | Orally, 3 times per week. | | Result: | A marked induction of COX-2 protein expression was detected by immunohistochemistry in the liver of CCl4-treated rats.
Significantly reduced the degree of liver fibrosis.
Dramatically suppressed α-SMA expression in CCl4-treated rats.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(248.89 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4889 mL | 12.4443 mL | 24.8886 mL | | 5 mM | 0.4978 mL | 2.4889 mL | 4.9777 mL | | 10 mM | 0.2489 mL | 1.2444 mL | 2.4889 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.22 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.22 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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