Name: Telacebec
Brand: Selleck Chemicals
SKU: S7739
Rating: 5 (1 reviews)

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

CAS: 1334719-95-7

Purity & Quality Control

Batch: Purity: 99.77%

99.77

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Choose Selective Bacterial Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT03563599	Completed	Treatment-naïve Sputum Smear-positive Patients With Drug-sensitive Pulmonary TB	Qurient Co. Ltd.	July 23 2018	Phase 2

References

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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