| Bioactivity | COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect[1]. |
| Invitro | COX-2-IN-30 (化合物 7a) 与 hCA 亚型结合，Ki 值分别为 183.4 nM (hCA I)、81.4 nM (hCA II)、38.4 nM (hCA IX)、21.6 nM (hCA XII)[1]。 |
| In Vivo | COX-2-IN-30 (化合物 7a) (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-30 (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。 COX-2-IN-30 显着降低 TNF-α 和 IL-1β 的水平[1]。COX-2-IN-30 (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-30 |
| Formula | C17H16N6O3S |
| Molar Mass | 384.41 |
| 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)benzenesulfonamide 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. |