4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸
中文名称 | 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 |
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中文同义词 | 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸;化合物GS-143 |
英文名称 | GS 143 |
英文同义词 | GS 143;4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid;4-(3-Benzyl-4-{[5-(2-fluorophenyl)furan-2-yl]methylidene}-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid;E2 conjugating enzyme,inhibit,IκBα,Th2,Ubiquitin conjugating enzyme,GS143,Ubiquitin ligase,IL-4,IκB kinase,βTrCP1,Nuclear factor-kappaB,eosinophil,Ubiquitin activating enzyme,Nuclear factor-κB,I kappa B kinase,NF-κB,E3 ligating enzyme,IKK,E1 activating enzyme,anti-asthma,E1/E2/E3 Enzyme,ubiquitination,Inhibitor,airway,inflammation;Benzoic acid, 4-[4-[[5-(2-fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]- |
CAS号 | 916232-21-8 |
分子式 | C28H19FN2O4 |
分子量 | 466.46 |
EINECS号 | |
相关类别 | |
Mol文件 | 916232-21-8.mol |
结构式 | ![]() |
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 性质
沸点 | 667.9±65.0 °C(Predicted) |
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密度 | 1.30±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMF:25.0(最大浓度 mg/mL);53.59(最大浓度 mM) DMF:PBS (pH 7.2) (1:4):0.2(最大浓度 mg/mL);0.43(最大浓度.mM) DMSO:31.38(最大浓度 mg/mL);67.28(最大浓度 mM) |
形态 | 结晶固体 |
酸度系数(pKa) | 4.20±0.10(Predicted) |
颜色 | 粉红至红色 |
IC50: 5.2 μM (SCF βTrCP1 -mediated IκBα ubiquitylation)
GS143 (10 μM or 20 μM) inhibits antigen-induced differentiation of Th2 cells but not of Th1 cells in vitro. The IL-4 production in Th2-polarizing condition is markedly suppressed by GS143 in a dose-dependent manner.
GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC
50
value of 10.5 μM. GS143 also inhibits TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC
50
value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC
50
values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin.
GS143 (16-32 μg/body; intranasal administration; once; BALB/c mice) treatment suppresses antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibits antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways.
Animal Model: | BALB/c mice (age 7-8weeks) injected with ovalbumin |
Dosage: | 16 μg/body or 32 μg/body |
Administration: | Intranasal administration; once |
Result: | Suppressed antigen-induced NF-κB activation in the lung of sensitized mice. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-110261 | GS143 | 1 mg | 400元 | |
2024/04/30 | HY-110261 | 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 GS143 | 916232-21-8 | 5mg | 1000元 |