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反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑
生物活性靶点体外研究体内研究 用途与合成方法 MSDS 反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑价格(试剂级) 上下游产品信息
| 中文名称 | 反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 |
|---|---|
| 中文同义词 | 反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑;反-4-[4-(4-氟苯基)-5-(2-甲氧基-4-嘧啶基)-1H-咪唑-1-基]环己醇;(1R,4R)-REL-4-(4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)-1H-咪唑-1-基)环己醇;化合物L-779450 |
| 英文名称 | SB 239063 |
| 英文同义词 | SB 239063;TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIDIMIDIN-4-YL)IMIDAZOLE;TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(4-FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE;TRANS-1-(4-HYDROXYCYCLOHEXYL)-4-(FLUOROPHENYL)-5-(2-METHOXYPYRIMIDIN-4-YL) IMIDAZOLE;TRANS-4-[4-(4-FLUOROPHENYL)-5-(2-METHOXY-4-PYRIMIDINYL)-1H-IMIDAZOL-1-YL]CYCLOHEXANOL;Cyclohexanol, 4-[4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]-, trans-;SB 239063 - CAS 798558-40-4 - Calbiochem;CS-402 |
| CAS号 | 193551-21-2 |
| 分子式 | C20H21FN4O2 |
| 分子量 | 368.4 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Protein Kinase Inhibitors and Activators |
| Mol文件 | 193551-21-2.mol |
| 结构式 |  |
反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 性质
| 熔点 | 206-207.2 °C |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：11 毫克/毫升 |
| 形态 | 白色固体 |
| 颜色 | 白色 |
| InChIKey | ZQUSFAUAYSEREK-WKILWMFISA-N |
反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 用途与合成方法
生物活性
SB239063是一种有效的选择性p38 MAPKα/β抑制剂，IC50为44 nM，对γ- 和 δ-激酶亚型没有活性。
靶点
| Target | Value |
| p38α (Cell-free assay) | 44 nM |
| p38β (Cell-free assay) | 44 nM |
体外研究
SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.
SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC
50
values of 120 nM and 350 nM, respectively.
Apoptosis Analysis
| Cell Line: | Eosinophils (guinea pig BALs) |
| Concentration: | 0.1μM, 1μM, 10μM |
| Incubation Time: | 29 hours, 47 hours |
| Result: | Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards. |
体内研究
SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia.
SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation.
SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC
50
of 5.8 mg/kg (2.8–10.3; 95% CL).
| Animal Model: | Male BALB/c mice (18–20 g) |
| Dosage: | 12 mg/kg |
| Administration: | Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days |
| Result: | Significantly inhibited the resultant antigen-induced airway eosinophilia. |
安全信息
| 安全说明 | 22-24/25 |
|---|---|
| WGK Germany | 3 |
| RTECS号 | GV9458000 |
| 海关编码 | 2933599590 |
MSDS信息
| 提供商 | 语言 |
|---|---|
SigmaAldrich | 英文 |
反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-11068 | 反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB 239063 | 193551-21-2 | 1mg | 500元 |
| 2024/08/19 | HY-11068 | 反式-1-(4-羟基环己基)-4-(4-氟苯基)-5-(2-甲氧基嘧啶-4-基)咪唑 SB 239063 | 193551-21-2 | 10mM * 1mLin DMSO | 892元 |
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