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;SC-560,COX-1抑制剂 |
| 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;生化试剂 |
| Mol文件 | 188817-13-2.mol |
| 结构式 |  |
5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑 性质
| 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 | 二甲基亚砜：>20mg/mL |
| 形态 | 类白色固体 |
| 酸度系数(pKa) | -3?+-.0.10(Predicted) |
| 颜色 | 白色至浅黄色至浅橙色 |
| Target | Value |
|
COX-1
(Cell-free assay) | 9 nM |
|
COX-2
(Cell-free assay) | 6.3 μM |
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.
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.
| 提供商 | 语言 |
|---|---|
|
英文
|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | C3572 | SC-560 SC-560 | 188817-13-2 | 25mg | 480元 |
| 2024/04/30 | HY-59105 | 5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑 SC-560 | 188817-13-2 | 10mM * 1mLin DMSO | 660元 |