| 產(chǎn)品描述： | Telacebec (Q203, IAP6) 是一種新型抗結(jié)核藥物，通過抑制分枝桿菌細(xì)胞色素 bc1 復(fù)合物來靶向結(jié)核分枝桿菌（Mycobacterium tuberculosis） 細(xì)胞能量的產(chǎn)生。Telacebec 對(duì)結(jié)核分枝桿菌 H37Rv 具有活性，在培養(yǎng)基中的 MIC50 為 2.7 nM |
| 靶點(diǎn)： |
Mycobacterium tuberculosis H37Rv:2.7 nM(MIC50);Antibacterial;?Antibiotic |
| 體外研究： |
Telacebec (Q203) inhibits the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range. |
| 體內(nèi)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. |
| 細(xì)胞實(shí)驗(yàn)： |
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. |
| 動(dòng)物實(shí)驗(yàn)： |
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 |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京