908568-01-4
908568-01-4 結(jié)構(gòu)式
基本信息
化合物 T24167
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
物理化學(xué)性質(zhì)
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)
常見問題列表
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. |