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1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑

用途

SC-58125 是一种有效的和选择性的环氧合酶 2 (COX-2) 的抑制剂,IC50 值为 0.04 μM。SC-58125 在体外和体内均表现出抗肿瘤活性,还可以抑制炎症部位的水肿并具有镇痛作用。

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名称

[ CAS 号 ]:
162054-19-5

[ 中文名 ]:
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑

[ 英文名 ]:
SC-58125

[英文别名 ]:

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

hCOX-2:0.04 μM (IC50)

hCOX-1:>100 μM (IC50)

[体外研究]

SC-58125(0.001-100μM)对COX-2(IC50=1μM)的诱导形式具有高度的选择性(IC50>100μM)[1]。SC-58125(10μM；20-140 s)是时间依赖性的,在1分钟内完成,在20秒时有一半的最大抑制作用[1]。SC-58125(25-100μM；3d)抑制HCA-7和LLC细胞的体外生长[3]。SC-58125(100µM；12 h)诱导LLC细胞G2阻滞[3]。SC-58125(25-100μM；3d)可降低HCA-7细胞p34cdc2水平[3]。SC-58125(100µM；24或72 h)不会诱导HCA-7和LLC细胞凋亡[3]。细胞增殖试验[3]细胞株：HCA-7和LLC细胞浓度：0、25、50、100μM孵育时间：3天结果：两种细胞系的细胞数和MTT活性均呈剂量依赖性降低。细胞周期分析[3]细胞系：LLC细胞浓度：100μM孵育时间：12小时结果：含4n DNA的细胞数量增加,呈剂量和时间依赖性。减少有丝分裂的数目。Western Blot分析[3]细胞系：HCA-7细胞浓度：0、25、50、100μM孵育时间：3天结果：p34cdc2活性呈剂量依赖性下降,抑制作用强,即使在最低浓度下。

[体内研究]

SC-58125(10mg/kg；每48h静脉注射)抑制小鼠结直肠癌异种移植瘤的生长[3]。SC-58125(10 mg/kg；单次静脉注射)可降低小鼠肿瘤PGE2水平[3]。SC-58125(10 mg/kg；单次静脉注射)不会改变小鼠体内COX-1和COX-2蛋白的肿瘤水平[3]。动物模型：裸鼠皮下注射HCA-7细胞[3]剂量：10mg/kg给药：每48h静脉注射一次；在肿瘤植入时或2周和4周后结果：显著降低肿瘤生长率。

[参考文献]

[1]. Gierse JK, et, al. A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors. J Biol Chem. 1996 Jun 28; 271(26): 15810-4.

[2]. Seibert K, et, al. Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain. Proc Natl Acad Sci U S A. 1994 Dec 6; 91(25): 12013-7.

[3]. Williams CS, et, al. A cyclooxygenase-2 inhibitor (SC-58125) blocks growth of established human colon cancer xenografts. Neoplasia. Sep-Oct 2001; 3(5): 428-36.

物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
512.6±50.0 °C at 760 mmHg

[ 分子式 ]:
C₁₇H₁₂F₄N₂O₂S

[ 分子量 ]:
384.348

[ 闪点 ]:
263.8±30.1 °C

[ 精确质量 ]:
384.055573

[ PSA ]:
60.34000

[ LogP ]:
3.86

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.573

[ 储存条件 ]:
-20°C，避光，干燥，密封

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

[ 海关编码 ]:
2933199090

海关

[ 海关编码 ]: 2933199090

[ 中文概述 ]:
2933199090. 其他结构上有非稠合吡唑环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933199090. other compounds containing an unfused pyrazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

The dual role of prostaglandin E(2) in excitotoxicity and preconditioning-induced neuroprotection.

Eur. J. Pharmacol. 517(1-2) , 17-27, (2005)

Cyclooxygenase-2 is harmful in models of cerebral ischemia yet plays a protective role in preconditioning-induced ischemic tolerance in the heart. This study examined the mechanisms underlying cycloox...

CpG oligodeoxynucleotides induce cyclooxygenase-2 in human B lymphocytes: implications for adjuvant activity and antibody production.

Clin. Immunol. 125(2) , 138-48, (2007)

Synthetic CpG oligodeoxynucleotides (ODN), similar to DNA sequences found in certain microorganisms, have shown promise as adjuvants for humans by enhancing immune responses. Since antibodies are ofte...

Cyclooxygenase-2 activity contributes to neuronal expression of cyclin D1 after anoxia/ischemia in vitro and in vivo.

Brain Res. Mol. Brain Res. 132(1) , 31-7, (2004)

Cyclooxygenase-2 (COX-2) activity has been implicated in the pathogenesis of neuronal cell death in ischemia and other diseases, but the mechanism by which COX-2 exacerbates cell death is unknown. COX...

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