Telacebec

Catalog No.S7739 Batch:S773902

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Technical Data

Formula

C29H28ClF3N4O2

Molecular Weight 557.01 CAS No. 1334719-95-7
Solubility (25°C)* In vitro Ethanol 8 mg/mL (14.36 mM)
DMSO 7 mg/mL (12.56 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.35mg/ml Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.35mg/ml Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 Assay:

[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 Study:

[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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.