IRAK4-IN-1 - IRAK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIRAK4-IN-1Cat. No.: HY-101922CAS No.: 1820787-94-7分式: CHNO分量: 337.42作靶点: IRAK作通路: Immunology/Inflammation; Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 14.29 m

2、g/mL (42.35 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 1.43 mg/mL (4.24 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 IRAK4-IN-1细胞介素-1 受体相关激酶 4 (IRAK4) 抑制剂，IC50 为 7 nM。IC50 & Target IC50: 7 nM (IRAK4) 1体外研究 The in vitro metabol

3、ic stability profiles of IRAK4-IN-1 (Compound 23) is measured, with EC50 of 2300 nM forthe rat whole blood (RWB) 1.体内研究 Oral pharmacokinetic studies of IRAK4-IN-1 (Compound 23) show it to have high bioavailability of 73% andlow plasma clearance(Clp=22 mL/min/kg) leading to a reasonable half-life of

4、1.3 h 1.PROTOCOLAnimal Rats 1Administration 1 In the TLR driven in vivo model, female Lewis rats are dosed with either vehicle or IRAK4-IN-1 (Compound23; 3, 10, 30, and 100 mg/kg; p.o.) dosed at 1 h prior to stimulation with Resiquimod, R848 (5 mg/kg, IP). At1.5 h post R848 stimulation, blood sample

5、s are obtained from the animals and cytokine levels are measured.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Smith GF, et al. Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation. Bioorg Med Chem Lett. 2017Jun 15;27(12):2721-2726.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 0