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Products > Immunology/Inflammation > Toll-like Receptor (TLR) > E6446 dihydrochloride (Synonyms: E-6446 dihydrochloride)
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Product name : E6446 dihydrochloride (Synonyms: E-6446 dihydrochloride)
Item : C2438
Price : 200mg, $1250;500mg, $2090; 1g, $2995; 2g, $4395
contact : Send inquiry to: info@acesobio.com
CAS : 1345675-25-3
Molecular Weight : 522.51
Formula : C₂₇H₃₇Cl₂N₃O₃
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order
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| Details: |
Description of:E6446 dihydrochloride(CAS:1345675-25-3)
E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM. IC50 value: 10 nM(HEK:TLR9 cell) [1] Target: TLRs inhibitor in vitro: E6446 potently inhibited IL-6 production induced by CpG2216 but was ineffective against induction by the TLR3 ligand poly inosine-cytosine. E6446 showed a modest but consistent superiority over AT791, and both were significantly more potent than hydroxychloroquine. Significantly, 250 nM and 1.25 μM E6446 completely suppressed all of the CpG oligo-induced changes in gene expression [1]. E6446 specifically inhibited TLR9 activation with CpG ODN 2006, in the range of 0.01–0.03 μM. A 100-fold higher concentration (2–8 μM) of E6446 was required to inhibit TLR7/8 activated by the imidazoquinoline compound R848 [2]. in vivo: To test their activity in vivo, mice were orally dosed with 20 mg/kg of AT791 or E6446 and 18 hours later were challenged with 60 μg CpG1668 oligonucleotide injected subcutaneously. CpG1668-induced IL-6 production was inhibited ~50% by AT791 and almost completely by E6446 [1]. therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection. Quality control data: Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS. Product will be shipped with supporting analytical data. 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.[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. |
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