| Identification | Back Directory | [Name]
E6446 (dihydrochloride) | [CAS]
1345675-25-3 | [Synonyms]
CS-2089
E6446 HCl
E6446 2HCl
E-6446 DihydrochL
E6446;E 6446;E-6446
E6446 hydrochloride
E6446 (dihydrochloride)
6-(3-(Pyrrolidin-1-yl)propoxy)-2-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)benzo[d]oxazole dihydrochloride | [Molecular Formula]
C27H36ClN3O3 | [MDL Number]
MFCD29472225 | [MOL File]
1345675-25-3.mol | [Molecular Weight]
486.05 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO:7.5(Max Conc. mg/mL);14.35(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);38.28(Max Conc. mM)
DMF:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.38(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);3.83(Max Conc. mM)
Water:100.0(Max Conc. mg/mL);191.38(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
E6446 is a synthetic antagonist of nucleic acid-sensing TLRs. , In vitro, low doses of E6446 specifically inhibited the activation of human and mouse TLR9. Tenfold higher concentrations of this compound also inhibited the human TLR8 response to single-stranded RNA. In vivo, therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection. Furthermore, severe signs of ECM, such as limb paralysis, brain vascular leak, and death, were all prevented by oral treatment with E6446. | [in vivo]
E6446 (20 mg/kg, p.o.) almost cmlpletely inhibits CpG1668-induced IL-6 production, and dose-dependently suppresses the development of ANA (anti-nuclear antibodies) in mice at 20 and 60 mg/kg[1]. E6446 (20, 60 mg/kg, p.o.) dose-dependently inhibits TLR9 signaling in mice. E6446 (60, 120 mg/kg, p.o.) prevents hyperresponsiveness of TLRs and LPS-induced septic shock in rodent malaria, diminishes TLR responsiveness during acute malaria, suppresses activation of both TLR7 and TLR9[2]. | [IC 50]
TLR7; TLR9 |
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