PeptideDB

Inflachromene

CAS: 908568-01-4 F: C21H19N3O4 W: 377.39

Inflachromene, a microglial inhibitor, binds to HMGB1 and HMGB2 and exerts anti-inflammatory effects. Inflachromene effe
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Bioactivity 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[1][2].
Target HMGB
Invitro 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[2].Inflachromene (1-10 μM) suppresses the increased levels of inflammation-related genes, such as Il6, Il1b, Nos2 and Tnf, after LPS stimulation[2].Inflachromene (5 μM) reduces LPS-induced secretion of the proinflammatory cytokine TNF-α[2].Inflachromene (5 μM; 30 min) substantially suppresses the nuclear translocation of NF-κB and the degradation of IκB[2].Inflachromene (1-10 μM; 30 min) inhibits LPS-induced phosphorylation of ERK, JNK and p38 MAPK in microglia[2].Inflachromene (10 μM; 30 min) completely prevents the death of cocultured neuroblastoma and primary neuronal cells by inhibiting microglia-mediated neurotoxicity[2].Inflachromene (1-10 μM; 24 h) has no significant effect on the viability of neurons[2].
In Vivo Inflachromene (2-10 mg/kg; i.p. once daily for 4 days) effectively blocks LPS-mediated microglial activation[2].Inflachromene (10 mg/kg; i.p. once daily for 30 days) significantly reduces the progression of disease, as determined by EAE clinical score[2].Inflachromene (1 mg/kg; i.v.) exhibits long half-life (14.1±6.43 h) and moderate Vss (2.02±1.02 L/kg)[1].Inflachromene (1 mg/kg; p.o.) exhibits high oral bioavailability (94%) and Cmax (0.59±0.16 g/mL)[1]. Animal Model:
Name Inflachromene
CAS 908568-01-4
Formula C21H19N3O4
Molar Mass 377.39
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Reference [1]. Lee HH, et, al. A validated UPLC-MS/MS method for pharmacokinetic study of inflachromene, a novel microglia inhibitor. J Pharm Biomed Anal. 2019 Mar 20; 166: 183-188. [2]. Lee S, et, al. A small molecule binding HMGB1 and HMGB2 inhibits microglia-mediated neuroinflammation. Nat Chem Biol. 2014 Dec; 10(12): 1055-60.