| Bioactivity | COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(Ki=48.9 nM) and hCA XII(Ki=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity[1]. |
| Invitro | 在碳酸酐酶抑制试验中，COX-2-IN-31 (compound 7b) 有效抑制 hCA IX 和 XII，Ki 值在纳摩尔范围内 (48.9 nM 和 5.8 nM)[1]。 |
| In Vivo | COX-2-IN-31 (compound 7b) (10 mg/kg; 口服; 单剂量) 表现出镇痛活性，同时显着减少小鼠的扭动次数[1]。COX-2-IN-31 (10 mg/kg; 口服; 单次剂量) 在 Carrageenan (HY-125474) 诱导的大鼠爪水肿试验中导致爪高度显着降低[1]。COX-2-IN-31 (10 mg/kg; 口服; 单剂量) 在雄性白化病大鼠的胃组织中表现出安全性[1]。 Animal Model: |
| Name | COX-2-IN-31 |
| Formula | C17H16N6O4S |
| Molar Mass | 400.41 |
| 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]. Ragab MA, et al. 4-(5-Amino-pyrazol-1-yl) benzene sulfonamide derivatives as novel multi-target anti-inflammatory agents endowed with inhibitory activity against COX-2, 5-LOX and carbonic anhydrase: Design, synthesis, and biological assessments. Eur J Med Chem. 2023 Mar 15; 250:115180. |