| Identification | Back Directory | [Name]
E6446 | [CAS]
1219925-73-1 | [Synonyms]
E6446
E 6446
(E6446)
E6446(free base)
Benzoxazole, 6-[3-(1-pyrrolidinyl)propoxy]-2-[4-[3-(1-pyrrolidinyl)propoxy]phenyl]- | [Molecular Formula]
C27H35N3O3 | [MDL Number]
MFCD28900679 | [MOL File]
1219925-73-1.mol | [Molecular Weight]
449.59 |
| Chemical Properties | Back Directory | [Boiling point ]
587.7±50.0 °C(Predicted) | [density ]
1.151±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
Ethanol:90.0(Max Conc. mg/mL);200.18(Max Conc. mM) | [form ]
Solid | [pka]
10.16±0.20(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD)[1][2][3]. | [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 | [storage]
Store at -20°C | [References]
[1] Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40. DOI:10.1124/mol.113.089821
[2] Franklin BS, et al. Therapeutical targeting of nucleic acid-sensing Toll-like receptors prevents experimental cerebral malaria. Proc Natl Acad Sci U S A. 2011 Mar 1;108(9):3689-94. DOI:10.1073/pnas.1015406108
[3] Wang W, et al. Identification of novel SCD1 inhibitor alleviates nonalcoholic fatty liver disease: critical role of liver-adipose axis. Cell Commun Signal. 2023 Sep 30;21(1):268. DOI:10.1186/s12964-023-01297-9 |
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