5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑

中文名称:

5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑

中文同义词:

5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑;COX-1抑制剂(SC-560);SC-560 SC-560;化合物SC560

英文名称:

SC-560

英文同义词:

SC-560;5-(4-CHLOROPHENYL)-1-(4-METHOXYPHENYL)-3-(TRIFLUOROMETHYL)-1H-PYRAZOLE;5-(4-CHLOROPHENYL)-1-(4-METHOXYPHENYL)-3-TRIFLUOROMETHYLPYRAZOLE;SC-560 Assay Reagent;1H-Pyrazole, 5-(4-chlorophenyl)-1-(4-Methoxyphenyl)-3-(trifluoroMethyl)-;5-(4-Chlorophenyl)-3-(trifluoromethyl)-1-(4-methoxyphenyl)-1H-pyrazole;5-(4-Chlorophenyl);SC-560 - CAS 188817-13-2 - Calbiochem

CAS号:

188817-13-2

分子式:

C17H12ClF3N2O

分子量:

352.74

EINECS号:

相关类别:

杂环类;医药中间体;合成;细胞生物学试剂

Mol文件:

188817-13-2.mol

熔点 

63 °C

沸点 

440.6±45.0 °C(Predicted)

密度 

1.33

储存条件 

2-8°C

溶解度 

DMSO: >20mg/mL

形态

Off-white solid

酸度系数(pKa)

-3?+-.0.10(Predicted)

生物活性

SC-560 是一种高度选择性的 COX-1 抑制剂，IC50值为9 nM，而对于 COX-2 的IC50值为6.3μM 比 COX-1 高近1,000倍。

靶点

Target Value COX-1 (Cell-free assay) 9 nM COX-2 (Cell-free assay) 6.3 μM

Target

Value

COX-1 (Cell-free assay)

9 nM

COX-2 (Cell-free assay)

6.3 μM

体外研究

Preincubation of COX-1 with SC-560 inhibits the conversion of arachidonic acid to PGE2 in a concentration-dependent manner. The IC 50 of SC-560 for COX-2 is 6.3 μM, nearly 1,000-fold higher than with COX-1. SC-560 shows a dose and time dependent inhibitory effect on HCC cell growth. SC-560 also inhibits colony formation in soft agar and induces apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreases the levels of the anti-apoptotic proteins survivin and XIAP and activates caspase 3 and 7 in a dose and time dependent fashion.

体内研究

Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2production, indicating that SC-560 is orally bioavailable and inhibits COX-1 in vivo . SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. The drug displays low less than 15% and formulation dependent bioavailability after oral administration and demonstrates kidney toxicity.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26-36

WGK Germany 

3