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4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑
生物活性靶点体外研究体内研究 用途与合成方法 MSDS 4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑价格(试剂级) 上下游产品信息
| 中文名称 | 4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑 |
|---|---|
| 中文同义词 | 4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑;RWJ 67657,P38Α和P38Β抑制剂 |
| 英文名称 | 4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol |
| 英文同义词 | 4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol;RWJ 67657;4-(4-Fluorophenyl)-2-(4-hydroxy-1-butynyl)-1-(3-phenylpropyl)-5-(4-Pyridyl)iMidazole;JNJ 3026582;RWJ-67657;JNJ-3026582;CS-1470;RWJ-67657; RWJ-67657; RWJ-67657;3-Butyn-1-ol, 4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]- |
| CAS号 | 215303-72-3 |
| 分子式 | C27H24FN3O |
| 分子量 | 425.5 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 215303-72-3.mol |
| 结构式 |  |
4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑 性质
| 熔点 | 124℃ |
|---|---|
| 沸点 | 611.8±65.0 °C(Predicted) |
| 密度 | 1.14±0.1 g/cm3(Predicted) |
| 储存条件 | Store at RT |
| 溶解度 | 乙醇中≤10mg/ml；DMSO 中≤5mg/ml；二甲基甲酰胺中≤2mg/ml |
| 酸度系数(pKa) | 14.37±0.10(Predicted) |
| 形态 | 黄色粉末 |
| 颜色 | 浅黄至黄色 |
4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑 用途与合成方法
生物活性
RWJ-67657 (JNJ 3026582) 是一种具有口服活性的选择性 p38α 和 p38β 抑制剂，IC50 分别为 1 和 11 μM。RWJ-67657 对 p38γ 和 p38δ 无活性，是心脏保护剂，具有抗炎和抗肿瘤活性。
靶点
p38α 1 μM (IC 50) | p38β 11 μM (IC 50) |
体外研究
RWJ-67657 inhibits the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells with an IC
50
of 3 nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B, with an IC
50
value of 13 nM.
RWJ67657 (10 μM; 24 hours) decreases colony formation in MCF-7 cells.
Cell Proliferation Assay
| Cell Line: | MCF-7 breast carcinoma cells |
| Concentration: | 10 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased colony formation. |
体内研究
RWJ-67657 inhibits TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration.
RWJ-67657 (50 mg/kg; administered orally; once per day for 7 consecutive days) displays a potent anti-inflammatory effect. By both improving the functioning of endothelial progenitor cells (EPCs) and reducing inflammation, EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke.
| Animal Model: | The db/db mice (male, 8 weeks old) with EPCs |
| Dosage: | 50 mg/kg |
| Administration: | Administered orally; once per day for 7 consecutive days |
| Result: | Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation. |
安全信息
MSDS信息
4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)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-15505 | 4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑 RWJ-67657 | 215303-72-3 | 5mg | 800元 |
| 2024/08/19 | HY-15505 | 4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑 RWJ-67657 | 215303-72-3 | 10mM * 1mLin DMSO | 880元 |
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