SC-236

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SC-236  纯度: 99.45%

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。

SC-236

SC-236 Chemical Structure

CAS No. : 170569-86-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1200 In-stock
25 mg ¥2500 In-stock
50 mg ¥4500 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model[1][2][3][4][5].

IC50 & Target[5]

COX-2

10 nM (IC50)

COX-1

17.8 μM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

SC-236 (6 mg/kg, gavage) exhibits anti-fibrotic properties in CCl4- treated animals[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

401.79

Formula

C16H11ClF3N3O2S

CAS 号

170569-86-5

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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (248.89 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

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, 6 months; -20°C, 1 month。-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。

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); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.22 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Shao-Yu Fang, et al. Reduction in MicroRNA-4488 Expression Induces NFκB Translocation in Venous Endothelial Cells Under Arterial Flow. Cardiovasc Drugs Ther. 2020 Sep 9.

    [2]. Anna Planagumà, et al. The selective cyclooxygenase-2 inhibitor SC-236 reduces liver fibrosis by mechanisms involving non-parenchymal cell apoptosis and PPARgamma activation. FASEB J. 2005 Jul;19(9):1120-2.

    [3]. Benjamin Chun-Yu Wong, et al. Cyclooxygenase-2 inhibitor (SC-236) suppresses activator protein-1 through c-Jun NH2-terminal kinase. Gastroenterology. 2004 Jan;126(1):136-47.

    [4]. Su-Jin Kim, et al. The COX-2 inhibitor SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model. Life Sci. 2007 Aug 23;81(11):863-72.

    [5]. T D Penning, et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). J Med Chem. 1997 Apr 25;40(9):1347-65.

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