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 4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑试剂级价格

CAS号:215303-72-3
英文名:4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol
中文名: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
CBNumber:CB52518847
分子式:C27H24FN3O
分子量:425.5
MOL File:215303-72-3.mol

4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑化学性质

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 :≤10mg/ml in ethanol;5mg/ml in DMSO;2mg/ml in dimethyl formamide
酸度系数(pKa) :14.37±0.10(Predicted)
形态 :Yellow powder.

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、用途与生产工艺

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.