Q203

SKU: orb1301821

Description

Telacebec (Q203) is a potent small-molecule inhibitor targeting the cytochrome b subunit QcrB of Mycobacterium tuberculosis, exhibiting potent activity with an MIC50 of 2.7 nM against the H37Rv strain. It serves as a key research tool for investigating mycobacterial respiration and has demonstrated efficacy in both in vitro assays and in vivo mouse models of tuberculosis infection.

Research Area

Infectious Disease & Virology

Key Properties

• CAS Number: 1334719-95-7
• MW: 557.01
• Purity: 99.47% (May vary between batches)
• Formula: C₂₉H₂₈ClF₃N₄O₂
• SMILES: CCc1nc2ccc(Cl)cn2c1C(=O)NCc1ccc(cc1)N1CCC(CC1)c1ccc(OC(F)(F)F)cc1
• Target: Antibiotic,Antibacterial
• Solubility: H2O:Insoluble;DMSO:11 mg/mL (19.75 mM)

Bioactivity

• Target IC50:
  Mycobacterium tuberculosis H37Rv:2.7 nM (MIC50)
• In Vivo:
  Q203 had a bioavailability of 90% and a terminal half-life of 23.4 h. The volume of distribution was moderate (5.27 l per kg body weight), and the systemic clearance was low (4.03 ml/min/kg). It promoted a reduction in bacterial load of more than 90% at a dose of 10 mg per kg body weight, an effect comparable to that of bedaquiline or isoniazid .
• In Vitro:
  Q203 was active against the reference strain M. tuberculosis H37Rv at a minimum concentration required to inhibit the growth of 50% of organisms (MIC50) of 2.7 nM in culture broth medium and at an MIC50 of 0.28 nM inside macrophages . Verapamil increased the potency of Q203 against Mycobacterium tuberculosis both in vitro and ex vivo . Inhibition of cytochrome bd, a parallel branch of the mycobacterial respiratory chain, by aurachin D invoked bactericidal activity of Q203. Inhibition of respiratory chain activity by Q203 was incomplete, but could be enhanced by inactivation of cytochrome bd, either by genetic knock-out or by inhibition with aurachin D .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bacterial, Antibiotic, IAP 6, IAP6, IAP-6, Inhibitor, inhibit, Q 203, Q203, Q-203, tuberculosis, Telacebec

Compound Identifiers

PubChem CID

68234908