Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Enpatoran (M5049) 是一种口服有效的TLR7/8选择性抑制剂,在HEK293 细胞中,IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran 在体内具有良好的药代动力学特性。Enpatoran 在先天性和适应性自身免疫阻断方面有研究的价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,260 | 现货 | ||
5 mg | ¥ 2,480 | 现货 | ||
10 mg | ¥ 3,730 | 现货 | ||
25 mg | ¥ 6,380 | 现货 | ||
50 mg | ¥ 8,590 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,750 | 现货 |
产品描述 | 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. |
靶点活性 | TLR8:24.1 nM, TLR7:11.1 nM |
体外活性 | 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[1]. |
体内活性 | 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[1]. |
分子量 | 320.31 |
分子式 | C16H15F3N4 |
CAS No. | 2101938-42-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 24.44 mg/mL (76.30 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.122 mL | 15.6099 mL | 31.2198 mL | 78.0494 mL |
5 mM | 0.6244 mL | 3.122 mL | 6.244 mL | 15.6099 mL | |
10 mM | 0.3122 mL | 1.561 mL | 3.122 mL | 7.8049 mL | |
20 mM | 0.1561 mL | 0.7805 mL | 1.561 mL | 3.9025 mL | |
50 mM | 0.0624 mL | 0.3122 mL | 0.6244 mL | 1.561 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Enpatoran 2101938-42-3 Immunology/Inflammation TLR inhibit M5049 Inhibitor Toll-like Receptor (TLR) M-5049 autoimmunity M 5049 TLR7/8 selective inhibitor