ETX1975-3
ETX1975-3 is an orally active inhibitor and bactericide targeting the bd cytochrome oxidase of Mycobacterium tuberculosis. ETX1975-3 disrupts electron transfer between the b-heme centers of the target enzyme, and in combination with Q203 (HY-101040), exerts bactericidal activity against both replicating and non-replicating Mycobacterium tuberculosis, and reduces bacterial loads in acute mouse models. ETX1975-3 retains activity against clinical isolates of multidrug-resistant/extensively drug-resistant Mycobacterium tuberculosis and non-tuberculous mycobacteria, while possessing favorable preclinical ADMET properties. ETX1975-3 can be used in studies related to tuberculosis and non-tuberculous mycobacterial infections.
For research use only. We do not sell to patients.
- Formula: C20H16ClFN4
- Molecular Weight:366.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
ETX1975-3 (3 μM) exhibits favorable in vitro ADMET properties, with low metabolic stability in mouse and human liver microsomes, low Caco-2 permeability, and high plasma protein binding rate in mice[1].
ETX1975-3 (1.7-5.0 μM; 15 h-5 days) targets the cytochrome bd oxidase in Mycobacterium abscessus ΔqcrCAB, with an IC50 of 1.7 μM for ATP depletion and an MIC50 of 5.0 μM[1].
ETX1975-3 exerts a synergistic antibacterial effect with Q203 (100 nM), with IC50 values of 1.4 μM, 0.5 μM, and 1.5 μM against cytochrome bd oxidase in Mycobacterium bovis BCG, Mycobacterium tuberculosis H37Rv, and Mycobacterium avium, respectively (ATP depletion assay)[1].
Combination treatment with ETX1975-3 (0.6-40 μM; 4 d) and 250 nM Q203 dose-dependently reduces the load of Mycobacterium tuberculosis N0145 in THP-1 macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ADME parameters in Caco-2 cells
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Concentration:/
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Incubation Time:/
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Result:Exhibited low metabolic clearance (MLM and HLM ≤2.0 μl/min/mg), extremely low intestinal permeability (Caco2 Papp ≤3×10-6 cm/s), and high plasma protein binding (>99.9%) in in vitro ADME assays.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tuberculosis infected model in BALB/cJ mice (female, 6-8 weeks old, intranasal infection with Mycobacterium tuberculosis N0145)[1]
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Dosage:50 mg/kg
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Administration:p.o.; once daily for 5 consecutive days per week; 2 weeks
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Result:Became moribund by day 9 post-treatment and required sacrifice at day 10.
Produced a statistically significant reduction in lung bacillary loads when combined with Q203 compared to Q203 alone.
Chemical Information
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Molecular Weight 366.82
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Formula C20H16ClFN4
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SMILES
CC1=NN2C3=CC(F)=CC=C3C(N[C@@H]4[C@H](C4)C5=CC=C(C=C5)Cl)=NC2=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ETX1975-3 Related Classifications
HY-181286 Related Classifications
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