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

生物活性靶点体外研究体内研究 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)苯甲酸试剂级价格

CAS号:916232-21-8
英文名:GS 143
中文名: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
CBNumber:CB64721604
分子式:C28H19FN2O4
分子量:466.46
MOL File:916232-21-8.mol

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)苯甲酸化学性质

沸点 :667.9±65.0 °C(Predicted)
密度 :1.30±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMF:25.0(Max Conc. mg/mL);53.59(Max Conc. mM)
DMF:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.43(Max Conc. mM)
DMSO:31.38(Max Conc. mg/mL);67.28(Max Conc. mM)
形态 :A crystalline solid
酸度系数(pKa) :4.20±0.10(Predicted)
颜色 :Pink to red

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、用途与生产工艺

生物活性 GS143 是一种选择性的 IκBα 泛素化抑制剂，对于 SCFβTrCP1 介导的 IκBα 泛素化作用的 IC50 为 5.2 μM。GS143 抑制靶基因的 NF-κB 活化和转录，并且不抑制蛋白酶体的活性，并具有抗哮喘作用。
靶点

IC50: 5.2 μM (SCF ^βTrCP1 -mediated IκBα ubiquitylation)
体外研究

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.

体内研究

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.