产品
编 号：F752900
分子式：C18H18O4
分子量：298.34
分子式：C18H18O4
分子量：298.34
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 24533-47-9
产品详情
生物活性：
L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3?μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
体内研究：
L6H21 (10 mg/kg, Oral gavage, daily) effectively inhibits EtOH + LPS-induced hepatic fat accumulation, hepatic steatosis and liver injury. L6H21 (0-40 mg/kg, Orally, daily for 4 weeks) attenuates metabolic disturbance, restores cognition and attenuates brain pathologies dose and time-dependently in HFD-fed rats, and shows neuroprotective effect in a model of prediabetes.Animal Model:Male C57BL6 mice (8-10 weeks old, n = 36, 8 mice in each group, 25-30 g, with EtOH and LPS)
Dosage:10 mg/kg
Administration:Oral gavage, daily, before EtOH feeding
Result:Decreased hepatic triglyceride (TG) concentration, markedly decreased serum alanine transaminase (ALT) and aspartate transaminase (AST) levels; Significantly decreased inflammation in liver tissue induced by EtOH + LPS.
Animal Model:Male Wistar rats (6-7 weeks old, 250 g, a normal diet (ND) (n=8) or a high-fat diet (HFD) (n=104) for 16?weeks)
Dosage:0, 10, 20, and 40 mg/kg
Administration:Orally, daily for 1, 2 or 4 weeks
Result:Ameliorated brain mitochondrial dysfunction in HFD-fed rats at 2-week administration time point; improved brain mitochondrial function in a dose-dependent manner for 4 weeks. Reduced hippocampal apoptosis in prediabetes for 4 weeks. Attenuated the reduction of dendritic spine volume and density for 4 weeks. Preserved microglial morphology in a dose-dependent manner.
体外研究：
L6H21 (10 μM, 2 h) inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells.L6H21 (10 μM, 2 h) attenuates EtOH + LPS-induced ROS formation and TLR4–NF-κB activation, and decreases NLRP3 inflammasome activation.
L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3?μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
体内研究：
L6H21 (10 mg/kg, Oral gavage, daily) effectively inhibits EtOH + LPS-induced hepatic fat accumulation, hepatic steatosis and liver injury. L6H21 (0-40 mg/kg, Orally, daily for 4 weeks) attenuates metabolic disturbance, restores cognition and attenuates brain pathologies dose and time-dependently in HFD-fed rats, and shows neuroprotective effect in a model of prediabetes.Animal Model:Male C57BL6 mice (8-10 weeks old, n = 36, 8 mice in each group, 25-30 g, with EtOH and LPS)
Dosage:10 mg/kg
Administration:Oral gavage, daily, before EtOH feeding
Result:Decreased hepatic triglyceride (TG) concentration, markedly decreased serum alanine transaminase (ALT) and aspartate transaminase (AST) levels; Significantly decreased inflammation in liver tissue induced by EtOH + LPS.
Animal Model:Male Wistar rats (6-7 weeks old, 250 g, a normal diet (ND) (n=8) or a high-fat diet (HFD) (n=104) for 16?weeks)
Dosage:0, 10, 20, and 40 mg/kg
Administration:Orally, daily for 1, 2 or 4 weeks
Result:Ameliorated brain mitochondrial dysfunction in HFD-fed rats at 2-week administration time point; improved brain mitochondrial function in a dose-dependent manner for 4 weeks. Reduced hippocampal apoptosis in prediabetes for 4 weeks. Attenuated the reduction of dendritic spine volume and density for 4 weeks. Preserved microglial morphology in a dose-dependent manner.
体外研究：
L6H21 (10 μM, 2 h) inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells.L6H21 (10 μM, 2 h) attenuates EtOH + LPS-induced ROS formation and TLR4–NF-κB activation, and decreases NLRP3 inflammasome activation.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备