| Bioactivity | TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury[1]. |
| Formula | C22H21ClF2N4O |
| Molar Mass | 430.88 |
| 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]. Jiang YY, et al., Discovery of pyrazolo[1,5-a]pyrimidine derivatives targeting TLR4-TLR4∗ homodimerization via AI-powered next-generation screening. Eur J Med Chem. 2024 Oct 6;280:116945. |