Telacebec (Q203)

Catalog No.S7739 Synonyms: IAP6

For research use only.

Telacebec (Q203, IAP6) 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 (Q203) Chemical Structure

CAS No. 1334719-95-7

Purity & Quality Control

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Biological Activity

Description Telacebec (Q203, IAP6) 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

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>

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>

Protocol (from reference)

Cell Research:

[2]

  • 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. 

Animal Research:

[2]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 557.01
Formula

C29H28ClF3N4O2

CAS No. 1334719-95-7
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03563599 Completed Drug: Telacebec (Q203)|Drug: Rifafour e-275 Treatment-naïve Sputum Smear-positive Patients With Drug-sensitive Pulmonary TB Qurient Co. Ltd. July 23 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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