HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
体内研究
HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis.
HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL.
HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human.
HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively.
Animal Model:
A rat model of collagen induced arthritis (CIA).
Dosage:
15, 50, 150 mg/kg.
Administration:
PO, once daily.
Result:
Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.
分子式
C21H24F3N5O2
分子量
435.44
CAS号
2410393-15-4
运输条件
Room temperature in continental US; may vary elsewhere.