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Inflachromene

目录号: PL08388 纯度: ≥99%

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。

CAS No. :908568-01-4

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中文名称	Inflachromene
英文名称	Inflachromene
英文别名	Inflachromene;AOB6225;5,12b-Dihydro-10-hydroxy-7,7-dimethyl-2-phenyl-1H,7H-[1]benzopyrano[4,3-c][1,2,4]triazolo[1,2-a]pyridazine-1,3(2H)-dione (ACI);ICM
Cas No.	908568-01-4
分子式	C₂₁H₁₉N₃O₄
分子量	377.39
包装储存	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)

产品详情	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。
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.
性状	Solid
IC50 & Target[1][2]	HMGB
体外研究(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. 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.
体内研究(In Vivo)	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 V ss (2.02±1.02 L/kg). Inflachromene (1 mg/kg; p.o.) exhibits high oral bioavailability (94%) and C max (0.59±0.16 g/mL). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	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)
参考文献	[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (264.98 mM; Need ultrasonic)配制储备液

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