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Chemical Structure| 1334719-95-7 Chemical Structure| 1334719-95-7

Structure of Telacebec
CAS No.: 1334719-95-7

Chemical Structure| 1334719-95-7

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Q203 is an inhibitor of mycobacterium tuberculosis cytochrome bc1, a bacterial enzyme complex needed for respiration.

Synonyms: Q203; IAP6

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Product Details of Telacebec

CAS No. :1334719-95-7
Formula : C29H28ClF3N4O2
M.W : 557.01
SMILES Code : O=C(C1=C(CC)N=C2C=CC(Cl)=CN21)NCC3=CC=C(N4CCC(C5=CC=C(OC(F)(F)F)C=C5)CC4)C=C3
Synonyms :
Q203; IAP6
MDL No. :MFCD28502122
InChI Key :OJICYBSWSZGRFB-UHFFFAOYSA-N
Pubchem ID :68234908

Safety of Telacebec

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mycobacterium bovis BCG 1.25 nM 24 hours To assess the effect of Telacebec on fadD26 promoter activity, showing a significant reduction in promoter activity Microorganisms. 2023 Sep 30;11(10):2469
Murine bone marrow-derived macrophages 0.2 nM and 2 nM 3 days and 7 days To evaluate the inhibitory effect of Telacebec on the metabolic activity of intracellular M. leprae. Results showed that 2 nM Telacebec inhibited ≈97% of metabolic activity in 3 days, and 0.2 nM Telacebec inhibited ≈40% of metabolic activity in 7 days. Emerg Infect Dis. 2022 Mar;28(3):749-751
Extracellular Mycobacterium leprae 0.2 nM and 2 nM 3 days and 7 days To evaluate the inhibitory effect of Telacebec on the metabolic activity of M. leprae. Results showed that 0.2 nM Telacebec inhibited ≈90% of metabolic activity in 3 days, and 2 nM Telacebec inhibited ≈99.9% of metabolic activity in 3 days. Emerg Infect Dis. 2022 Mar;28(3):749-751
Mycobacterium smegmatis CIII2CIV2 53 ± 19 nM 3 hours To investigate the inhibitory effect of Telacebec on CIII2CIV2, results showed an IC50 of 53 ± 19 nM. Elife. 2021 Sep 30;10:e71959
Mycobacterium bovis BCG 10 nM 7 hours To evaluate the effect of Telacebec on protein expression in BCG, revealing 15 proteins upregulated and 26 proteins downregulated, particularly those involved in PDIM/PGL biosynthesis Microorganisms. 2023 Sep 30;11(10):2469
Mycobacterium smegmatis bd-KO 100 nM, 1 µM, 10 µM 96 hours Evaluate the effect of Q203 on the growth of M. smegmatis bd-KO, results showed Q203 significantly extended the lag phase but the strain eventually resumed growth Int J Mol Sci. 2022 Sep 7;23(18):10331
Mycobacterium smegmatis WT 100 nM, 1 µM, 10 µM 96 hours Evaluate the effect of Q203 on the growth of M. smegmatis WT, results showed no significant impact on WT strain growth Int J Mol Sci. 2022 Sep 7;23(18):10331

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Mouse footpad infection model Oral gavage 0.5, 2, 5, 10 mg/kg 5 days per week for 1-4 weeks Evaluate the therapeutic effect of Telacebec alone or in combination with rifampin in a mouse footpad infection model. Results showed that Telacebec alone rendered most mouse footpads culture negative in 2 weeks, and combining Telacebec with rifampin resulted in a relapse-free cure 24 weeks after completing 2 weeks of treatment. Antimicrob Agents Chemother. 2020 May 21;64(6):e00259-20
Athymic nude mice Mouse foot pad model of infection Gavage 2 mg/kg 1 dose, 5 consecutive daily doses, or 20 doses (5 days × 4 weeks) To evaluate the bactericidal efficacy of Telacebec in a mouse foot pad model of infection. Results showed that 1 or 5 consecutive doses of Telacebec significantly reduced bacterial viability, indicating a faster in vivo bactericidal efficacy of Telacebec. Emerg Infect Dis. 2022 Mar;28(3):749-751
Mice Acute tuberculosis model Oral Q203: 5 mg/kg, ND-011992: 25 mg/kg 5 consecutive days Evaluate the efficacy of ND-011992 in combination with Q203 in an acute tuberculosis model EMBO Mol Med. 2021 Jan 11;13(1):e13207.
Mice Acute tuberculosis model Oral 5 mg/kg 5 consecutive days Evaluate the efficacy of ND-011992 in combination with Q203 in a mouse model of tuberculosis EMBO Mol Med. 2021 Jan 11;13(1):e13207.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06481163 Buruli Ulcer PHASE2 ACTIVE_NOT_RECRUITING 2025-12-25 Barwon Health, Geelong, Victor... More >>ia, 3220, Australia|Royal Melbourne Hospital, Melbourne, Australia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

8.98mL

1.80mL

0.90mL

17.95mL

3.59mL

1.80mL

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