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Inflachromene

Catalog No. T24167 CAS 908568-01-4

Synonyms: ICM

Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.Inflachromene reduces seizure severity in a mouse model of epilepsy by inhibiting HMGB1 translocation, inhibits endothelial proliferation through the HMGB1/2-regulated TLR4-NF-κB pathway, and inhibits autophagy by regulating Beclin 1 activity. Inflachromene can be used to study epilepsy.

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Inflachromene, CAS 908568-01-4

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1 mg	In stock	$ 199.00

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Purity: 99.88%

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Description	Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.Inflachromene reduces seizure severity in a mouse model of epilepsy by inhibiting HMGB1 translocation, inhibits endothelial proliferation through the HMGB1/2-regulated TLR4-NF-κB pathway, and inhibits autophagy by regulating Beclin 1 activity. Inflachromene can be used to study epilepsy.
In vitro	In BV-2 microglial cells, Inflachromene efficiently blocks LPS-induced nitrite release in a dose-dependent manner (0.01-100 μM; 24 h) without any toxicity[1]. After LPS stimulation, Inflachromene (1-10 μM) suppresses the increased levels of inflammation-related genes, such as Il6, Il1b, Nos2, and Tnf[1]. At a concentration of 5 μM, Inflachromene reduces LPS-induced secretion of the proinflammatory cytokine TNF-α[1]. In microglia, Inflachromene (5 μM; 30 min) substantially suppresses the nuclear translocation of NF-κB and the degradation of IκB[1]. The phosphorylation of ERK, JNK, and p38 MAPK in microglia induced by LPS is inhibited by Inflachromene (1-10 μM; 30 min)[1]. In the co-culture of neuroblastoma and primary neuronal cells, Inflachromene (10 μM; 30 min) completely prevents the death by inhibiting microglia-mediated neurotoxicity[1].There is no significant effect on the viability of neurons with Inflachromene (1-10 μM; 24 h)[1].
In vivo	In a dose-dependent manner (2-10 mg/kg; i.p. once daily for 4 days), Inflachromene effectively blocks LPS-mediated microglial activation[1]. For a duration of 30 days (10 mg/kg; i.p. once daily), Inflachromene significantly reduces the progression of disease, as determined by EAE clinical score[1]. When administered intravenously (i.v.) at a dose of 1 mg/kg, Inflachromene exhibits a long half-life (14.1±6.43 h) and moderate Vss (2.02±1.02 L/kg)[2]. Given orally (p.o.) at a dose of 1 mg/kg, Inflachromene shows high oral bioavailability (94%) and Cmax (0.59±0.16 g/mL)[2].

Synonyms	ICM
Molecular Weight	377.39
Formula	C21H19N3O4
CAS No.	908568-01-4

Storage

keep away from direct sunlight,keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (211.98 mM), Sonication is recommended.

References and Literature

1. Lee S, et, al. A small molecule binding HMGB1 and HMGB2 inhibits microglia-mediated neuroinflammation. Nat Chem Biol. 2014 Dec; 10(12): 1055-60. 2. 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. 3. Cho W, Koo JY, Park Y, Oh K, Lee S, Song JS, Bae MA, Lim D, Lee DS, Park SB. Treatment of Sepsis Pathogenesis with High Mobility Group Box Protein 1-Regulating Anti-inflammatory Agents. J Med Chem. 2017 Jan 12;60(1):170-179. doi: 10.1021/acs.jmedchem.6b00954. Epub 2016 Dec 21. PubMed PMID: 28001381. 4. Block ML. Neuroinflammation: modulating mighty microglia. Nat Chem Biol. 2014 Dec;10(12):988-9. doi: 10.1038/nchembio.1691. PubMed PMID: 25393492.

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Keywords

Inflachromene 908568-01-4 Others ICM inhibitor inhibit

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