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GSK3186899

CAS No. : 1972617-87-0

MCE 国际站：GSK3186899

产品活性：GSK3186899 (DDD-853651) 是 CRK12 的一个抑制剂，其对 L. donovani 的 EC₅₀ 值为 1.4 μM。

研究领域：Anti-infection

作用靶点：Parasite

In Vitro: GSK3186899 (Compound 7) is active against L. donovani in an intra-macrophage assay with an EC₅₀ value of 1.4 μM, and shows good selectivity against mammalian THP-1 host cells (EC₅₀ value>50 μM). This is not as potent as reported data for amphotericin B (EC₅₀ value of 0.07 μM in the intra-macrophage assay), but is comparable to the clinically used drugs miltefosine and paromomycin (EC₅₀ values of 0.9 μM and 6.6 μM, respectively). GSK3186899 is also active in cidal axenic amastigote assay (EC₅₀ value of 0.1 μM). At a concentration of 0.2 μM, GSK3186899 is cytocidal at 96 h; increasing the concentration to 1.8 μM reduced this time to 48 h. GSK3186899 demonstrates a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is also more active in a panel of Leishmania lines using human peripheral blood mononuclear cells as the host cells.

In Vivo: In the mouse model of infection, GSK3186899 demonstrates comparable activity to the front-line drug miltefosine, reducing parasite levels by 99% when dosed orally twice a day for 10 days at 25 mg/kg. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). The non-clinical safety data for GSK3186899 suggests a suitable therapeutic window for progression into regulatory preclinical studies. Non-GLP preclinical assessment of cardiovascular effects and genotoxicity does not reveal any issues that would prevent further development. In addition, there are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested. Both the in vivo efficacy and safety profile of GSK3186899 support progression to definitive safety studies.

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