| Bioactivity | NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively[1]. |
| Target | IC50: 70 nM (Trypanosoma brucei), 0.16 μM (CYP1A2), 0.42 μM (CYP2C19) |
| In Vivo | NPD-2975 (25 mg/kg，每日2次，连用5天；灌胃) 提高了 HAT 感染小鼠模型中 i 期的存活率[1]。NPD-2975 在小鼠中的药代动力学分析[1]Route |
| Name | NPD-2975 |
| Formula | C14H13FN4O |
| Molar Mass | 272.28 |
| 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]. Zheng Y, et al. Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy. J Med Chem. 2023 Aug 10;66(15):10252-10264. |