炎性色素
- CAS号:908568-01-4
- 英文名:Inflachromene
- 中文名:炎性色素
- CBNumber:CB94200546
- 分子式:C21H19N3O4
- 分子量:377.39
- MOL File:908568-01-4.mol
- 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(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) - 形态 :A crystalline solid
- 酸度系数(pKa) :9.65±0.40(Predicted)
- 颜色 :White to yellow
炎性色素性质、用途与生产工艺
- 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。
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靶点
HMGB
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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.
- 更新日期:2024/04/30
- 产品编号:HY-113772
- 产品名称:Inflachromene
- CAS编号:
- 包装:1 mg
- 价格:1590元
- 更新日期:2024/04/30
- 产品编号:HY-113772
- 产品名称:炎性色素 Inflachromene
- CAS编号:908568-01-4
- 包装:5mg
- 价格:3500元
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:CAYMAN
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- 国家:美国
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- 公司名称:United States Biological Inc.
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- 电子邮件:chemicals@usbio.net
- 国家:美国
- 产品数:6256
- 优势度:80
- 公司名称:MedChemExpress
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- 国家:美国
- 产品数:6398
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