E6742 | TLR7/8 inhibitor | Probechem Biochemicals

Chemical Structure : E6742

CAS No.: 1700609-11-5

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E6742 (E 6742)

货号: 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	￥3580	In stock
10 mg	￥5480	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	383.430
分子式	C20H22FN5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

E6742 (E 6742)

生物&药学活性

物理化学性质&存储条件

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E6742 (E 6742)

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物理化学性质&存储条件

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