2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. 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.

ETX1975-3

ETX1975-3 Chemical Structure

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ETX1975-3 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

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[1].

In Vitro

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.

ETX1975-3 Related Antibodies

Cell Viability Assay[1]

Cell Line: ADME parameters in Caco-2 cells
Concentration: /
Incubation Time: /
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.
Parmacokinetics
Species Dose Route Bioavailability Tmax T1/2 Cmax AUClast CL Vss
Mice[1] 2 mg/kg i.v. / / 2.23 h 927.53 ng/mL 593.67 ng·h/mL 53.3 mL/min/kg 5.58 L/kg
Mice[1] 10 mg/kg p.o. 44 % 1.00 h 2.21 h 392 ng/mL 1312 ng·h/mL / /
In Vivo

ETX1975-3 (50 mg/kg; p.o.; once daily, 5 days per week; 2 weeks) fails to reduce the pulmonary bacterial load of Mycobacterium tuberculosis N0145 in BALB/cJ mice; however, when combined with Q203, it significantly decreases the pulmonary bacillary load in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tuberculosis infected model in BALB/cJ mice (female, 6-8 weeks old, intranasal infection with Mycobacterium tuberculosis N0145)[1]
Dosage: 50 mg/kg
Administration: p.o.; once daily for 5 consecutive days per week; 2 weeks
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.
Molecular Weight

366.82

Formula

C20H16ClFN4
SMILES

CC1=NN2C3=CC(F)=CC=C3C(N[C@@H]4[C@H](C4)C5=CC=C(C=C5)Cl)=NC2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ETX1975-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ETX1975-3Cytochrome P450CYPsMycobacterium bovis BCGcytochrome bd oxidaseMycobacterium aviumnontuberculous mycobacteriaMycobacterium abscessusTHP-1 macrophagesBALB/cJ miceMycobacterium tuberculosisMycobacterium tuberculosis N0145Mycobacterium tuberculosis H37RvInhibitorinhibitorinhibit

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