炎性色素
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- CAS号:
- 908568-01-4
- 英文名:
- Inflachromene
- 英文别名:
- ICM;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;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-
- 中文名:
- 炎性色素
- 中文别名:
- 炎性色素;化合物 T24167
- CBNumber:
- CB94200546
- 分子式:
- C21H19N3O4
- 分子量:
- 377.39
- MOL File:
- 908568-01-4.mol
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炎性色素化学性质
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沸点:
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532.6±60.0 °C(Predicted)
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密度:
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1.50±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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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)-
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形态:
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A crystalline solid
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酸度系数(pKa):
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9.65±0.40(Predicted)
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颜色:
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White to yellow
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炎性色素性质、用途与生产工艺
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。
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).
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Animal Model:
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Male C57BL/6 mice (11 weeks; 25-30 g) are treated with LPS
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Dosage:
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2, 10 mg/kg
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Administration:
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I.p. once daily for 4 days
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Result:
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Blocked LPS-mediated microglial activation, even at a dose of 2 mg/kg.
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Animal Model:
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Sprague-Dawley (SD) rats (7 weeks; 230-250 g)
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Dosage:
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1 mg/kg (Pharmacokinetic Analysis)
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Administration:
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I.v. and p.o. administration
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Result:
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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.
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炎性色素
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-113772 | Inflachromene | | 1 mg | 1590元 |
| 2024/08/19 | HY-113772 | 炎性色素
Inflachromene | 908568-01-4 | 5mg | 3500元 |
908568-01-4, 炎性色素 相关搜索:
- 炎性色素
- 化合物 T24167
- 908568-01-4
- 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-
- ICM
- Inflachromene
- 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)