炎性色素
| 中文名称 | 炎性色素 |
|---|---|
| 中文同义词 | 化合物 T24167;炎性色素 |
| 英文名称 | Inflachromene |
| 英文同义词 | 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;Inflachromene;ICM;1H,7H-[1]Benzopyrano[4,3-c][1,2,4]triazolo[1,2-a]pyridazine-1,3(2H)-dione, 5,12b-dihydro-10-hydroxy-7,7-dimethyl-2-phenyl- |
| CAS号 | 908568-01-4 |
| 分子式 | C21H19N3O4 |
| 分子量 | 377.39 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 908568-01-4.mol |
| 结构式 |  |
炎性色素 性质
| 沸点 | 532.6±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.50±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF:30.0(最大浓度 mg/mL);79.49(最大浓度 mM) DMSO:30.0(最大浓度 mg/mL);79.49(最大浓度 mM) DMSO:PBS ( pH 7.2) (1:4):0.2(最大浓度 mg/mL);0.53(最大浓度 mM) 乙醇:2.5(最大浓度 mg/mL);6.62(最大浓度 mM) |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 9.65±0.40(Predicted) |
| 颜色 | 白色至黄色 |
HMGB
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.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-113772 | Inflachromene | 1 mg | 1590元 | |
| 2024/04/30 | HY-113772 | 炎性色素 Inflachromene | 908568-01-4 | 5mg | 3500元 |