Home Microbiology Bacterial inhibitor Telacebec For research use only.

Telacebec

Synonyms: Q203，IAP6

Telacebec is a novel antituberculosis drug that targets Mycobacterium tuberculosis cellular energy production through inhibition of the mycobacterial cytochrome bc1 complex. Telacebec (Q203, IAP6) is active against Mycobacterium tuberculosis H37Rv with MIC50 of 2.7 nM in culture broth medium.

Telacebec Chemical Structure

Telacebec Chemical Structure

CAS No. 1334719-95-7

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Biological Activity

Description Telacebec is a novel antituberculosis drug that targets Mycobacterium tuberculosis cellular energy production through inhibition of the mycobacterial cytochrome bc1 complex. Telacebec (Q203, IAP6) is active against Mycobacterium tuberculosis H37Rv with MIC50 of 2.7 nM in culture broth medium.
Targets
Mycobacterium tuberculosis H37Rv [2]
2.7 nM(MIC50)
In vitro
In vitro

Telacebec (Q203) inhibits the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range.<sup><a class="sref" href="#s_ref">[1]</a></sup><sup><a class="sref" href="#s_ref">[2]</a></sup>
Cell Research 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 <i>M. tuberculosis</i> 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. 
In Vivo
In vivo

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.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03563599 Completed
Treatment-naïve Sputum Smear-positive Patients With Drug-sensitive Pulmonary TB
Qurient Co. Ltd.
 July 23 2018 Phase 2

Chemical Information & Solubility

Molecular Weight 557.01 Formula

C29H28ClF3N4O2
CAS No. 1334719-95-7 SDF --
Smiles CCC1=C([N]2C=C(Cl)C=CC2=N1)C(=O)NCC3=CC=C(C=C3)N4CCC(CC4)C5=CC=C(OC(F)(F)F)C=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 20 mg/mL ( (35.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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