4-(5-(4-氯苯基)-3-(三氟甲基)-1H-
- CAS号:170569-86-5
- 英文名:4-[5-(4-CHLOROPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]BENZENESULFONAMIDE
- 中文名:4-(5-(4-氯苯基)-3-(三氟甲基)-1H-
- CBNumber:CB3243082
- 分子式:C16H11ClF3N3O2S
- 分子量:401.79
- MOL File:Mol file
- 熔点 :146-148°C
- 沸点 :543.4±60.0 °C(Predicted)
- 密度 :1.54±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: >20mg/mL
- 形态 :powder
- 酸度系数(pKa) :9.66±0.10(Predicted)
- 颜色 :white to off-white
4-(5-(4-氯苯基)-3-(三氟甲基)-1H-性质、用途与生产工艺
- 生物活性 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。
-
靶点
COX-2
10 nM (IC 50 )
COX-1
17.8 μM (IC 50 )
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体外研究
SC-236 (15 μM, 30 min) suppresses the side effects of NSAIDs and prevented inflammation in vECs subjected to ALSS.
SC-236 significantly induces PPARγ expression in HSCs and acted as a potent PPARγ agonist in a luciferase-reporter trans-activation assay.
SC-236 strongly inhibits, in a time- and concentration-dependent manner, macrophage viability.
SC-236, either alone or in combination with 15d-PGJ2, induced a marked pro-apoptotic effect in HSCs in culture.
SC-236 mediates antitumor effect by modulation of AP-1-signaling pathway.
Western Blot Analysis
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
Cell Line: COS 7 cells. Concentration: 3 and 10 μM. Incubation Time: 18 h (combined with 15d-PGJ 2 ). Result: Acted in a concentration-dependent manner as a PPARγ agonist. -
体内研究
SC-236 (6 mg/kg, gavage) exhibits anti-fibrotic properties in CCl4- treated animals.
Animal Model: Seventy-six male adult Wistar rats weighing 200-220 g (CCl 4 -treated). 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.
- 更新日期：2024/11/08
- 产品编号：HY-W010983
- 产品名称：4-(5-(4-氯苯基)-3-(三氟甲基)-1H- SC-236
- CAS编号：170569-86-5
- 包装：5mg
- 价格：800元
- 更新日期：2024/11/08
- 产品编号：HY-W010983
- 产品名称：4-(5-(4-氯苯基)-3-(三氟甲基)-1H- SC-236
- CAS编号：170569-86-5
- 包装：10mM * 1mLin DMSO
- 价格：880元
- 公司名称：TORONTO
- 联系电话：--
- 电子邮件：info@trc-canada.com
- 国家：加拿大
- 产品数：6038
- 优势度：71
