Inflachromene
目录号 : KM10896 CAS No. : 908568-01-4 纯度 : ≥96%

Inflachromene 是一种小胶质细胞抑制剂,可与 HMGB1 和 HMGB2 结合并发挥抗炎作用。Inflachromene 有效下调 HMGB 的促炎功能并减少神经元损伤。Inflachromene 可用于神经炎性疾病的研究。

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5mg
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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.

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.
分子式
C21N3O4H19
分子量
377.39
CAS号
908568-01-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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