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Chemical Structure : E6742
Catalog No.: PC-21010Not For Human Use, Lab Use Only.
E6742 (E6742) is a potent, selective, dual TLR7/8 inhibitor with binding Kd of 1.7 uM/37 nM in ITC assays, respectively, inhibits TLR7/8 agonist CL097 induced reporter activation with IC50 values of 22, 68, and 3.0 nM for hTLR7, mTLR7, and hTLR8, respectively.
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E6742 (E6742) is a potent, selective, dual TLR7/8 inhibitor with binding Kd of 1.7 uM/37 nM in ITC assays, respectively, inhibits TLR7/8 agonist CL097 induced reporter activation with IC50 values of 22, 68, and 3.0 nM for hTLR7, mTLR7, and hTLR8, respectively.
E6742 does not inhibit TLR9-mediated NF-κB activation at concentrations at >30 uM, also shows no effect on stimulation of TLR2, 3, 4, or 5.
E6742 potently inhibits IL-6 and IFN-α production stimulated by TLR7/8 agonist SL4-Ig with IC50 of 5.0 and 2.0 nM, respectively.
E6742 completely suppressed arthritis at 200 mg/kg and significantly reduced symptoms at 33 mg/kg in the pristane-induced murine model of SLE.
E6742 suppressed increase in autoantibodies and blocked the advance of organ damage in mouse models of lupus.
| M.Wt | 383.430 | |
| Formula | C20H22FN5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sally T Ishizaka, et al. Eur J Pharmacol. 2023 Aug 4;175962.
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