E6742 | TLR7/8 inhibitor | Probechem Biochemicals

Chemical Structure : E6742

CAS No.: 1700609-11-5

E6742 (E 6742)

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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5 mg	$358	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	383.430
Formula	C20H22FN5O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2R,6R)-4-(8-cyanoquinolin-5-yl)-N-((3S,4R)-4-fluoropyrrolidin-3-yl)-6-methylmorpholine-2-carboxamide

References

1. Sally T Ishizaka, et al. Eur J Pharmacol. 2023 Aug 4;175962.

E6742 (E 6742)

Biological Activity

Physicochemical Properties

References

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