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Telacebec Bacterial inhibitor

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

Cat.No.S7739

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

Chemical Structure

Molecular Weight: 557.01

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Quality Control

Batch: Purity: 99.77%

99.77

Related Targets	Integrase Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease
Other Bacterial Products	Berberine BTZ043 Racemate Teicoplanin Ornidazole Skatole Berberine Sulfate Pipemidic acid Ceftiofur PBTZ169 Aminothiazole

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (35.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (0.63mM)	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 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (0.63mM)	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.

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.

Chemical Information, Storage & Stability

Molecular Weight	557.01	Formula	C₂₉H₂₈ClF₃N₄O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1334719-95-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Q203，IAP6			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

Mechanism of Action

Targets/IC₅₀/Ki	Mycobacterium tuberculosis H37Rv 2.7 nM(MIC50)
In vitro	This compound (Q203) inhibits the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range.
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>
References	[1] https://pubmed.ncbi.nlm.nih.gov/32212527/ [2] https://pubmed.ncbi.nlm.nih.gov/23913123/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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