Telacebec

Catalog No.S7739 Batch:S773901

Technical Data

Formula	C₂₉H₂₈ClF₃N₄O₂
Molecular Weight	557.01	CAS No.	1334719-95-7
Solubility (25°C)*	In vitro	DMSO	20 mg/mL (35.9 mM)
		Ethanol	20 mg/mL (35.9 mM)
		Water	Insoluble
* <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.<a class="sref" href="#s_ref">[1]</a><a class="sref" href="#s_ref">[2]</a>

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.<a class="sref" href="#s_ref">[2]</a>

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

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 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.

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

References

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SHIPPING AND STORAGE
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