| 产品描述： | Telacebec (Q203, IAP6) 是一种新型抗结核药物，通过抑制分枝杆菌细胞色素 bc1 复合物来靶向结核分枝杆菌（Mycobacterium tuberculosis） 细胞能量的产生。Telacebec 对结核分枝杆菌 H37Rv 具有活性，在培养基中的 MIC50 为 2.7 nM |
| 靶点： |
Mycobacterium tuberculosis H37Rv:2.7 nM(MIC50);Antibacterial; Antibiotic |
| 体外研究： |
Telacebec (Q203) inhibits the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range. |
| 体内研究： |
Telacebec (Q203) is efficacious in a mouse model of tuberculosis at a dose less than 1 mg/kg body weight and displays pharmacokinetic and safety profiles compatible with once-daily dosing. |
| 细胞实验： |
Cell lines: Raw 264.7 cells Concentrations: 0.1 nM-100 µM Incubation Time: -- Method: Telacebec (Q203) are incubated with macrophages previously. Raw 264.7 cells (American Type Culture Collection TIB-71) were infected with M. tuberculosis H37Rv-GFP at a multiplicity of infection of 2:1 and dispensed into plates. After 5 d of infection, macrophages were stained with Syto 60 for Image acquisition. |
| 动物实验： |
Animal Models: A high dose of M. tuberculosis H37Rv infected-acute tuberculosis BALB/c mouse model Dosages: 0.4, 2, 10 mg/kg Administration: Oral gavage |
| 参考文献： |
1. Veronique R de Jager, et al. Telacebec (Q203), a New Antituberculosis Agent. N Engl J Med. 2020 Mar 26;382(13):1280-1281. 2. Kevin Pethe, et al. Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. Nat Med. 2013 Sep;19(9):1157-60. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.795 ml |
8.977 ml |
17.953 ml |
| 5 mM |
0.359 ml |
1.795 ml |
3.591 ml |
| 10 mM |
0.18 ml |
0.898 ml |
1.795 ml |
| 50 mM |
0.036 ml |
0.18 ml |
0.359 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京