Inflachromene

Research use only, not for human use.

Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.

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.

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 (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.

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908568-01-4

377.39

C21H19N3O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (264.98 mM; Ultrasonic )

CC1(C)Oc2cc(O)ccc2C2C1=CCn1n2c(=O)n(-c2ccccc2)c1=O

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(-20℃)

With Ice Pack

≥ 2 years