For research use only. Not for therapeutic Use.
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[1].
HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis[1].
HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL[1].
HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human[1].
HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively[1].
| Catalog Number | I045441 |
| CAS Number | 2410393-15-4 |
| Synonyms | N-[2-[2-(dimethylamino)ethyl]-6-(2-hydroxypropan-2-yl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide |
| Molecular Formula | C21H24F3N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H24F3N5O2/c1-20(2,31)14-11-16-13(12-29(27-16)9-8-28(3)4)10-17(14)26-19(30)15-6-5-7-18(25-15)21(22,23)24/h5-7,10-12,31H,8-9H2,1-4H3,(H,26,30) |
| InChIKey | QAOWCAZEVIIQTF-UHFFFAOYSA-N |
| SMILES | CC(C)(C1=CC2=NN(C=C2C=C1NC(=O)C3=NC(=CC=C3)C(F)(F)F)CCN(C)C)O |
| Reference | [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. |
