上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
GSK3186899 (Synonyms: DDD-853651)
GSK3186899 (DDD-853651) 是 CRK12 的一个抑制剂,其对 L. donovani 的 EC50 值为 1.4 μM。
GSK3186899 Chemical Structure
CAS No. : 1972617-87-0
规格 | 是否有货 | ||
---|---|---|---|
100 mg | 询价 | ||
250 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
生物活性 |
GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay. |
IC50 & Target |
CRK12[1]. |
---|---|
体外研究 (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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
体内研究 (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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
Clinical Trial |
|
分子量 |
491.53 |
Formula |
C19H28F3N7O3S |
CAS 号 |
1972617-87-0 |
运输条件 |
Room temperature in continental US; may vary elsewhere. |
储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务