| Description | HS271 is a selective, highly potent and orally active IRAK4 inhibitor (IC50= 7.2 μM). HS271 shows excellent enzymatic and cellular activities, as well as excellent pharmacokinetic properties. |
| In vivo | 在大鼠的LPS诱导的TNFα产生和胶原诱导关节炎模型中, HS271 (15-150 mg/kg) 表现出强效的抗炎活性，其半衰期为3.3小时，最大血浆浓度(Cmax)达到2107 ng/mL。HS271在小鼠、大鼠、犬和猴的口服生物利用度分别为67.3%、58.2%、14.4%和49%[1]。 |
| Target activity | IRAK4:7.2 μM (IC50) |
| molecular weight | 435.44 |
| Molecular formula | C21H24F3N5O2 |
| CAS | 2410393-15-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90 mg/mL (206.7 mM), Sonication is recommended. |
| References | 1. Wenqiang Zhai, et al. Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors. Bioorg Med Chem Lett. 2020 Nov 24;31:127686. |