4-(5-(4-氯苯基)-3-(三氟甲基)-1H-

4-(5-(4-氯苯基)-3-(三氟甲基)-1H-

中文名称4-(5-(4-氯苯基)-3-(三氟甲基)-1H-
中文同义词4-(5-(4-氯苯基)-3-(三氟甲基)-1H-;4-(5-(4-氯苯基)-3-(三氟甲基)-1H-吡唑-1-基)苯磺酰胺
英文名称4-[5-(4-CHLOROPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]BENZENESULFONAMIDE
英文同义词SC-236;4-[5-(4-CHLOROPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]BENZENESULFONAMIDE;4-[5-(4-CHLOROPHENYL)-3-(TRIFLUOROMETHYL)PYRAZOL-1-YL]BENZENESULFONAMIDE;SC-58236;Benzenesulfonamide, 4-[5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-;SC 236 - SC 58236;SC-236,gastric,PPAR,cancer,ischemia,Liver,inhibit,allodynia,Inhibitor,fibrogenesis,neuroprotection,COX,Cyclooxygenase,Apoptosis,TNF-α,Peroxisome proliferator-activated receptors,fibrosis,SC236
CAS号170569-86-5
分子式C16H11ClF3N3O2S
分子量401.79
EINECS号
相关类别Amines;Apoptosis;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer compounds;Pharmaceuticals
Mol文件Mol File
结构式4-(5-(4-氯苯基)-3-(三氟甲基)-1H- 结构式

4-(5-(4-氯苯基)-3-(三氟甲基)-1H- 性质

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
溶解度二甲基亚砜:>20mg/mL
形态粉末
酸度系数(pKa)9.66±0.10(Predicted)
颜色白色至类白色

4-(5-(4-氯苯基)-3-(三氟甲基)-1H- 用途与合成方法

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。

COX-2

10 nM (IC 50 )

COX-1

17.8 μM (IC 50 )

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.

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.

安全信息

危险品标志T
危险类别码25
安全说明45
危险品运输编号UN 2811 6.1 / PGIII
WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-W0109834-(5-(4-氯苯基)-3-(三氟甲基)-1H-
SC-236
170569-86-55mg800元
2024/04/30HY-W0109834-(5-(4-氯苯基)-3-(三氟甲基)-1H-
SC-236
170569-86-510mg1200元

4-(5-(4-氯苯基)-3-(三氟甲基)-1H- 上下游产品信息

"4-(5-(4-氯苯基)-3-(三氟甲基)-1H-"相关产品信息
SC75741 SC-1 ALPHA,ALPHA-二苯基-4-[(3-吡啶亚甲基)氨基]-1-吡嗪戊腈 魚藤素 6-甲基萘乙酸 5-溴-2-(4-氟苯基)-3-(4-甲基磺酰基苯基)噻吩 右旋酮洛芬 萘普生 甲氯灭酸钠 5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑 硫化舒林酸 布洛芬 菲尼酮 R-布洛芬 美洛昔康 抑制剂 吲哚美辛 吡罗昔康
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