| Bioactivity | IRAK4-IN-19 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 4.3 nM. IRAK4-IN-19 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-19 can be used for researching arthritis disease[1]. |
| Invitro | IRAK4-IN-19 (compound 39) has inhibitory activity against LPS-induced IL23 in THP and DC with IC50s of 0.23 and 0.22 μM, respectively[1]. |
| In Vivo | IRAK4-IN-19 (30 mg/kg; twice daily for 21 days) completely stops arthritis development in arthritis rats at 30 mg/kg[1].IRAK4-IN-19 (1 mg/kg for IV, 5 mg/kg for PO, single dosage) exhibits a favorable pharmacokinetics profile[1].IRAK4-IN-19 (5, 15, 45 and 75 mg/kg) exhibits good efficacy in an acute mouse model for the IL-1β induced IL-6 expression, with 64% inhibition at 75 mg/kg dose, 37% inhibition at 45 mg/kg dose, 16% inhibition at 15 mg/kg dose and 9% inhibition at 5 mg/kg[1]. Animal Model: |
| Name | IRAK4-IN-19 |
| Formula | C25H26F2N8O |
| Molar Mass | 492.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Chen Y, et al. Bicyclic pyrimidine compounds as potent IRAK4 inhibitors. Bioorg Med Chem Lett. 2022 Jul 18:128900. |