Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Enpatoran (M5049) hydrochloride is a potent and orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively. This compound specifically inhibits TLR7 and TLR8, while showing no activity against TLR3, TLR4, and TLR9. Enpatoran hydrochloride has the ability to block both synthetic molecule ligands and natural endogenous RNA ligands. Additionally, it demonstrates excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be a valuable tool for studying and modulating both innate and adaptive autoimmunity. [1]
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,470 | 5日内发货 | ||
5 mg | ¥ 2,490 | 5日内发货 | ||
10 mg | ¥ 4,280 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,730 | 5日内发货 |
Enpatoran hydrochloride 的其他形式现货产品:
产品描述 | Enpatoran (M5049) hydrochloride is a potent and orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively. This compound specifically inhibits TLR7 and TLR8, while showing no activity against TLR3, TLR4, and TLR9. Enpatoran hydrochloride has the ability to block both synthetic molecule ligands and natural endogenous RNA ligands. Additionally, it demonstrates excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be a valuable tool for studying and modulating both innate and adaptive autoimmunity. [1] |
靶点活性 | TLR8:24.1 nM (IC50), TLR7:11.1 nM (IC50) |
体外活性 | Enpatoran hydrochloride (0.01 nM-10 μM) inhibits production of IL-6 stimulated by all the ligands (miR-122, Let7c RNA, Alu RNA, and R848) with IC50 values ranging from 35 to 45 nM[1]. |
体内活性 | Pre-treatment with Enpatoran hydrochloride (oral gavage; 1 mg/kg) before R848 (intraperitoneal injection of 25 μg) dose-dependently inhibits the production of IL-6 and IFN-α in mice[1]. Enpatoran hydrochloride exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg)[1]. Enpatoran hydrochloride exhibits moderate half-lives (mouse 1.4, rat 5.0 and dog 13 h) due to high plasma clearance (1.4, 1.2 and 0.59 L/h/kg, respectively) combined with large volumes of distribution (2.7, 8.7 and 5.7 L/kg, respectively) following intravenous administration (mouse, rat and dog 1.0 mg/kg)[1]. |
分子量 | 356.78 |
分子式 | C16H16ClF3N4 |
CAS No. | 2101945-93-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16.67 mg/mL (46.72 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8028 mL | 14.0142 mL | 28.0285 mL | 70.0712 mL |
5 mM | 0.5606 mL | 2.8028 mL | 5.6057 mL | 14.0142 mL | |
10 mM | 0.2803 mL | 1.4014 mL | 2.8028 mL | 7.0071 mL | |
20 mM | 0.1401 mL | 0.7007 mL | 1.4014 mL | 3.5036 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 hydrochloride 2101945-93-9 Enpatoran Hydrochloride Inhibitor inhibitor inhibit