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Inflachromene 

目录号: HY-113772 纯度: >96.0%
产品使用指南

Inflachromene 是一种小胶质细胞抑制剂,可与 HMGB1HMGB2 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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Inflachromene Chemical Structure

Inflachromene Chemical Structure

CAS No. : 908568-01-4

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Description

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].

IC50 & Target

HMGB[2]

In Vitro

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: Male C57BL/6 mice (11 weeks; 25-30 g) are treated with LPS[2]
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)[1]
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.
Molecular Weight

377.39

Formula

C₂₁H₁₉N₃O₄

CAS No.

908568-01-4

SMILES

O=C1N(C2=CC=CC=C2)C(N3CC=C(C(C)(C)OC4=CC(O)=CC=C45)C5N31)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

References

Purity: >96.0%

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Keywords:

InflachromeneOthersmicroglialanti-inflammatoryHMGBneuronalInhibitorinhibitorinhibit

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产品名称:
Inflachromene
目录号:
HY-113772
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