HS271 (C09-1138-264)

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC 50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic propertiesIn VivoHS271 (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 t 1/2 of 3.3 h and C max 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:SolidIC50& Target:IRAK4 7.2 μM (IC 50 ). Specifications and Purity: 99%. Molecular Formula: C21H24F3N5O2. Molecular Weight: 435.44. PubChem CID: 146386401. Isomeric SMILES: CC(C)(C1=CC2=NN(C=C2C=C1NC(=O)C3=NC(=CC=C3)C(F)(F)F)CCN(C)C)O.