Enpatoran

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Enpatoran 是 TLR7 (IC50 = 11.1 nM) 和 TLR8 (IC50 = 24.1 nM) 的抑制剂。发现 Enpatoran 在体外和体内对 TLR3、TLR4 和 TLR9 没有活性。

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.(In Vitro):Enpatoran inhibited activity against different TLRs in a variety of cellular systems. Enpatoran potently inhibited TLR7 and TLR8 in HEK NF-κB-luciferase reporter cells with IC50 values in the low nanomolar range. Additionally, Enpatoran was found to be potent against TLR7 and TLR8 in PBMCs as well as whole blood. There appears to be an increased selectivity for TLR7 inhibition relative to TLR8 for Enpatoran in whole blood compared with PBMCs and transfected HEK cells.(In Vivo):In the BXSB-Yaa model, there is a robust increase in multiple autoantibodies, and Enpatoran significantly reduced both DNA-containing reactivities such as anti-dsDNA and anti-histones, as well as RNA-binding protein reactivities such as anti-RiboP and anti-SmRNP. At high dosages of Enpatoran, the effect on autoantibodies is so profound that titers are reduced below the baseline levels.

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Animal Model:Female C57BL/6 mice Dosage:0.1 mg/kg and 1 mg/kg Administration:Oral gavage; administered 1 hour prior to R848 challenge Result:The TLR7/8 agonist R848 stimulated both IFN-α and IL-6 production in mice. Enpatoran decreased IFN-α and IL-6 production stimulated by R848.Animal Model:Female CD1 mice, Female Wistar rats, Female beagle dogs Dosage:1 mg/kg (Pharmacokinetic Analysis) Administration:Intravenous (i.v.) or oral gavage Result:T1/2s of 1.4, 5.0 and 13 h for mice, rats and dogs, respectively.

M5049

Immunology/Inflammation

TLR

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2101938-42-3

320.31

C16H15F3N4

>98% (HPLC)

In Vitro:?Ethanol : 100 mg/mL (312.20 m)

N[C@H](C[C@@H](C1)C(F)(F)F)CN1c(c1cccnc11)ccc1C#N

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(-20℃)

With Ice Pack

≥ 2 years