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Q203

Catalog No. T5400   CAS 1334719-95-7
Synonyms: IAP6, Telacebec

Q203 (Telacebec) is a novel potent anti-tuberculosis agent targeting cytochrome b subunit qcrB and inhibits M. tuberculosis H37Rv (MIC50: 2.7 nM).

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Q203 Chemical Structure
Q203, CAS 1334719-95-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 59.00
5 mg In stock $ 162.00
10 mg In stock $ 252.00
25 mg In stock $ 453.00
50 mg In stock $ 667.00
100 mg In stock $ 949.00
1 mL * 10 mM (in DMSO) In stock $ 198.00
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Purity: 99.47%
Purity: 98.02%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Q203 (Telacebec) is a novel potent anti-tuberculosis agent targeting cytochrome b subunit qcrB and inhibits M. tuberculosis H37Rv (MIC50: 2.7 nM).
Targets&IC50 Mycobacterium tuberculosis H37Rv:2.7 nM (MIC50)
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 [1]. Verapamil increased the potency of Q203 against Mycobacterium tuberculosis both in vitro and ex vivo [2]. 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 [3].
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 [1].
Synonyms IAP6, Telacebec
Molecular Weight 557.01
Formula C29H28ClF3N4O2
CAS No. 1334719-95-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 18 mg/mL (32.3 mM)

H2O: Insoluble

TargetMolReferences and Literature

1. Pethe K, et al. Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. Nat Med. 2013 Sep;19(9):1157-60. 2. Jang J, et al. Efflux Attenuates the Antibacterial Activity of Q203 in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e02637-16. 3. Lu P, et al. The anti-mycobacterial activity of the cytochrome bcc inhibitor Q203 can be enhanced by small-molecule inhibition of cytochrome bd. Sci Rep. 2018 Feb 8;8(1):2625.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Infection Compound Library ReFRAME Related Library Anti-Viral Compound Library Clinical Compound Library Anti-Bacterial Compound Library Antibiotics Library

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Keywords

Q203 1334719-95-7 Microbiology/Virology Antibacterial Antibiotic Q-203 IAP-6 inhibit Bacterial IAP6 IAP 6 Q 203 Telacebec Inhibitor inhibitor

 

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