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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Treatment with varying concentrations of GW4064 (1, 2.5, 5, 10 μM) decreases lipid accumulation in cells. Specifically, GW4064 treatment notably reduces oleic acid-induced CD36 protein levels in a dose-dependent manner, indicating that the inhibition of CD36 expression is a key mechanism in preventing hepatic lipid accumulation[2]. |
体内研究 | GW4064 effectively suppresses weight gain in C57BL/6 mice on high-fat diets, including those with added cholesterol. It significantly mitigates diet-induced hepatic steatosis, as evidenced by reduced triglyceride and free fatty acid levels in the liver, and notably decreases CD36 expression without altering lipogenesis-related gene expressions. Additionally, GW4064 alleviates hepatic inflammation without impacting white adipose tissue[2]. In ANIT-treated rats, GW4064 administration (30 mg/kg) leads to substantial reductions in serum levels of ALT, AST, LDH, and ALP, and significantly lowers serum bile acid levels. Although bilirubin levels decrease, they do not reach statistical significance. Notably, GW4064 proves more effective in reducing these liver damage markers than TUDCA, which only reduces LDH levels[3]. |
体外研究 | Treatment with varying concentrations of GW4064 (1, 2.5, 5, 10 μM) decreases lipid accumulation in cells. Specifically, GW4064 treatment notably reduces oleic acid-induced CD36 protein levels in a dose-dependent manner, indicating that the inhibition of CD36 expression is a key mechanism in preventing hepatic lipid accumulation[2]. |
作用机制 | FXR has a structural conserved ligand-binding pocket with conformational flexibility to allow the binding of specific ligands. GW4064, as an FXR agonist, enters the FXR pocket and occupies a binding site to mediate the function of FXR. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
HEK293 cells | Function assay | Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.026 μM | 25305688 | ||
HEK293 cells | Function assay | Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50=0.07 μM | 17292610 | ||
HeLa cells | Function assay | 24 h | Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay, EC50=0.51 μM | 25934227 | |
human Caco-2 cells | 1 μM | Function assay | 6 days | Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR | 17963371 |
Dose | Mice: 20 mg/kg[3] (i.p.), 50 mg/kg[4] (i.p.); 2.5 mg/kg[5] (i.v.); 150 mg/kg[6] (p.o.) |
Administration | i.p., i.v., p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.84mL 0.37mL 0.18mL |
9.21mL 1.84mL 0.92mL |
18.42mL 3.68mL 1.84mL |
CAS号 | 278779-30-9 |
分子式 | C28H22Cl3NO4 |
分子量 | 542.838 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 105 mg/mL(193.43 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO DMF: 100 mg/mL(184.22 mM),配合低频超声助溶 |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear PO 0.5% CMC-Na 38 mg/mL suspension |