产品
编 号：F514964
分子式：C21H19N3O4
分子量：377.39
分子式：C21H19N3O4
分子量：377.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
询价
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10mg
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询价
结构图
CAS No: 908568-01-4
产品详情
生物活性：
Inflachromene, a microglial inhibitor, binds to HMGB1 and HMGB2 and exerts anti-inflammatory effects. Inflachromene effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage. Inflachromene can be used for the research of neuroinflammatory disorders.
体内研究：
Inflachromene (2-10 mg/kg; i.p. once daily for 4 days) effectively blocks LPS-mediated microglial activation.Inflachromene (10 mg/kg; i.p. once daily for 30 days) significantly reduces the progression of disease, as determined by EAE clinical score.Inflachromene (1 mg/kg; i.v.) exhibits long half-life (14.1±6.43 h) and moderate Vss (2.02±1.02 L/kg).Inflachromene (1 mg/kg; p.o.) exhibits high oral bioavailability (94%) and Cmax (0.59±0.16 g/mL).Animal Model:Male C57BL/6 mice (11 weeks; 25-30 g) are treated with LPS
Dosage:2, 10 mg/kg
Administration:I.p. once daily for 4 days
Result:Blocked LPS-mediated microglial activation, even at a dose of 2 mg/kg.
Animal Model:Sprague-Dawley (SD) rats (7 weeks; 230-250 g)
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:I.v. and p.o. administration
Result:I.v.: t1/2=14.1±6.43 h; CL= 0.14±0.01 L/kg/h; Vss=2.02±1.02 L/kg.P.o.: t1/2=7.96±1.16 h; F=94%; Cmax=0.59±0.16 g/mL.
体外研究：
Inflachromene (0.01-100 μM; 24 h) efficiently blocks LPS-induced nitrite release in a dose-dependent manner without any toxicity in BV-2 microglial cells.Inflachromene (1-10 μM) suppresses the increased levels of inflammation-related genes, such as Il6, Il1b, Nos2 and Tnf, after LPS stimulation.Inflachromene (5 μM) reduces LPS-induced secretion of the proinflammatory cytokine TNF-α.Inflachromene (5 μM; 30 min) substantially suppresses the nuclear translocation of NF-κB and the degradation of IκB.Inflachromene (1-10 μM; 30 min) inhibits LPS-induced phosphorylation of ERK, JNK and p38 MAPK in microglia.Inflachromene (10 μM; 30 min) completely prevents the death of cocultured neuroblastoma and primary neuronal cells by inhibiting microglia-mediated neurotoxicity.Inflachromene (1-10 μM; 24 h) has no significant effect on the viability of neurons.
Inflachromene, a microglial inhibitor, binds to HMGB1 and HMGB2 and exerts anti-inflammatory effects. Inflachromene effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage. Inflachromene can be used for the research of neuroinflammatory disorders.
体内研究：
Inflachromene (2-10 mg/kg; i.p. once daily for 4 days) effectively blocks LPS-mediated microglial activation.Inflachromene (10 mg/kg; i.p. once daily for 30 days) significantly reduces the progression of disease, as determined by EAE clinical score.Inflachromene (1 mg/kg; i.v.) exhibits long half-life (14.1±6.43 h) and moderate Vss (2.02±1.02 L/kg).Inflachromene (1 mg/kg; p.o.) exhibits high oral bioavailability (94%) and Cmax (0.59±0.16 g/mL).Animal Model:Male C57BL/6 mice (11 weeks; 25-30 g) are treated with LPS
Dosage:2, 10 mg/kg
Administration:I.p. once daily for 4 days
Result:Blocked LPS-mediated microglial activation, even at a dose of 2 mg/kg.
Animal Model:Sprague-Dawley (SD) rats (7 weeks; 230-250 g)
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:I.v. and p.o. administration
Result:I.v.: t1/2=14.1±6.43 h; CL= 0.14±0.01 L/kg/h; Vss=2.02±1.02 L/kg.P.o.: t1/2=7.96±1.16 h; F=94%; Cmax=0.59±0.16 g/mL.
体外研究：
Inflachromene (0.01-100 μM; 24 h) efficiently blocks LPS-induced nitrite release in a dose-dependent manner without any toxicity in BV-2 microglial cells.Inflachromene (1-10 μM) suppresses the increased levels of inflammation-related genes, such as Il6, Il1b, Nos2 and Tnf, after LPS stimulation.Inflachromene (5 μM) reduces LPS-induced secretion of the proinflammatory cytokine TNF-α.Inflachromene (5 μM; 30 min) substantially suppresses the nuclear translocation of NF-κB and the degradation of IκB.Inflachromene (1-10 μM; 30 min) inhibits LPS-induced phosphorylation of ERK, JNK and p38 MAPK in microglia.Inflachromene (10 μM; 30 min) completely prevents the death of cocultured neuroblastoma and primary neuronal cells by inhibiting microglia-mediated neurotoxicity.Inflachromene (1-10 μM; 24 h) has no significant effect on the viability of neurons.
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