908568-01-4

中文名称炎性色素

英文名称 Inflachromene

CAS 908568-01-4

分子式 C21H19N3O4

分子量 377.39

MOL 文件 908568-01-4.mol

908568-01-4 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

炎性色素
化合物 T24167

英文别名

Inflachromene
Inflachromene (ICM)
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

所属类别

生物化工：抑制剂

物理化学性质

沸点532.6±60.0 °C(Predicted)

密度1.50±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMF:30.0(Max Conc. mg/mL);79.49(Max Conc. mM)
DMSO:30.0(Max Conc. mg/mL);79.49(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.53(Max Conc. mM)
Ethanol:2.5(Max Conc. mg/mL);6.62(Max Conc. mM)

酸度系数(pKa)9.65±0.40(Predicted)

形态结晶固体

颜色White to yellow

常见问题列表

生物活性

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。

靶点

HMGB

体外研究

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.

体内研究

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).

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.: t _1/2 =14.1±6.43 h; CL= 0.14±0.01 L/kg/h; V _ss =2.02±1.02 L/kg. P.o.: t _1/2 =7.96±1.16 h; F=94%; C _max =0.59±0.16 g/mL.