2. Anti-infection
  3. Bacterial
  4. TBA-7371

TBA-7371 is an orally active and non-covalent inhibitor of Decaprenylphosphoryl-β-D-ribose oxidase (DprE1) of Mycobacterium tuberculosis (MIC=0.64 μg/mL). TBA-7371 can block the synthesis of arabinose in the bacterial cell wall, resulting in cell wall structural defects, thereby exerting an anti-tuberculosis effect. TBA-7371 can be used in the research of anti-tuberculosis drugs and has a synergistic bactericidal effect with Bedaquiline (HY-14881) and other drugs.

For research use only. We do not sell to patients.

TBA-7371 Chemical Structure

TBA-7371 Chemical Structure

CAS No. : 1494675-86-3

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Based on 1 publication(s) in Google Scholar

TBA-7371 Related Antibodies

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1 Publications Citing Use of MCE TBA-7371

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Description

TBA-7371 is an orally active and non-covalent inhibitor of Decaprenylphosphoryl-β-D-ribose oxidase (DprE1) of Mycobacterium tuberculosis (MIC=0.64 μg/mL). TBA-7371 can block the synthesis of arabinose in the bacterial cell wall, resulting in cell wall structural defects, thereby exerting an anti-tuberculosis effect. TBA-7371 can be used in the research of anti-tuberculosis drugs and has a synergistic bactericidal effect with Bedaquiline (HY-14881) and other drugs[1][2][3].

IC50 & Target

DprE1[1]
In Vitro

The MIC of TBA-7371 against Erdman and H37Rv strains of Mycobacterium tuberculosis is 1 μg/mL. In the presence of 4% human serum albumin, the MIC increases only 2-fold, indicating that binding to human serum albumin had little effect[2].
TBA-7371 (1, 10, 100 μg/mL; 14 days) shows dose-dependent bactericidal activity against Erdman strain of Mycobacterium tuberculosis, with the 100 μg/mL group showing the most significant bactericidal effect[2].

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

TBA-7371 Related Antibodies

Cell Viability Assay[1]

Cell Line: Mycobacterium tuberculosis Erdman
Concentration: 1 μg/mL, 10 μg/mL, 100 μg/mL
Incubation Time: 14 days
Result: All concentrations significantly reduced bacterial CFU counts over 14 days compared to the DMSO control, with the 100 μg/ml group showing the highest bactericidal activity, demonstrating dose-dependent killing.
In Vivo

TBA-7371 (100, 200 mg/kg; oral gavage; twice daily; 4-8 weeks) synergistically exerts bactericidal and fungicidal activity with Bedaquiline (HY-14881) and GSK2556286 (HY-147017) in the BALB/c mouse tuberculosis model[3].
TBA-7371 (50, 100, 200 mg/kg; oral gavage; twice daily; 8 weeks) significantly reduces bacterial burden in lung tissue after 8 weeks of treatment in the C3HeB/Fe J mouse tuberculosis model[3].

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

Animal Model: Female BALB/c mice (5-6 weeks old, specific pathogen-free) + subacute tuberculosis infection model induced by aerosol of Mycobacterium tuberculosis H37Rv[3]
Dosage: 100 mg/kg, 200 mg/kg (0.5% carboxymethylcellulose + 0.1% Tween 80)
Administration: Oral gavage, twice daily (8 h apart), 5 days/week for 4-8 weeks; Combination with Bedaquiline (25 mg/kg) and GSK2556286 (50 mg/kg) (BGA regimen)
Result: At 100 or 200 mg/kg bid significantly increased bactericidal activity after 8 weeks, with lung CFU counts of 1.48 (200 mg/kg) and 1.78 (100 mg/kg), demonstrating superior sterilizing activity compared to two-drug combinations.
Animal Model: Female C3HeB/FeJ mice (8-10 weeks old, specific pathogen-free) + chronic tuberculosis infection model with caseous necrotic pulmonary lesions induced by aerosol of Mycobacterium tuberculosis Erdman[3]
Dosage: 50 mg/kg, 100 mg/kg, 200 mg/kg (0.5% carboxymethylcellulose + 0.1% Tween 80)
Administration: Oral gavage, twice daily, 5 days/week for 8 weeks
Result: After 8 weeks, all dose groups showed significant reduction in lung bacterial burden compared to untreated controls.
The 100 and 200 mg/kg groups achieved approximately 1.5 log CFU reduction, with dose-dependent efficacy.
At 100 mg/kg bid exhibited consistent bactericidal activity, with higher drug retention in caseous lesions at trough concentrations.
Clinical Trial
Molecular Weight

355.39

Formula

C18H21N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(CC2=NC=NC(OC)=C2C)C3=CC(C)=CN=C31)NCCO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (70.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8138 mL 14.0691 mL 28.1381 mL
5 mM 0.5628 mL 2.8138 mL 5.6276 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8138 mL 14.0691 mL 28.1381 mL 70.3453 mL
5 mM 0.5628 mL 2.8138 mL 5.6276 mL 14.0691 mL
10 mM 0.2814 mL 1.4069 mL 2.8138 mL 7.0345 mL
15 mM 0.1876 mL 0.9379 mL 1.8759 mL 4.6897 mL
20 mM 0.1407 mL 0.7035 mL 1.4069 mL 3.5173 mL
25 mM 0.1126 mL 0.5628 mL 1.1255 mL 2.8138 mL
30 mM 0.0938 mL 0.4690 mL 0.9379 mL 2.3448 mL
40 mM 0.0703 mL 0.3517 mL 0.7035 mL 1.7586 mL
50 mM 0.0563 mL 0.2814 mL 0.5628 mL 1.4069 mL
60 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 mL
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TBA-7371 Related Classifications

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:

TBA-73711494675-86-3TBA7371TBA 7371BacterialDprE1noncovalentantitubercularantituberculosistuberculosisInhibitorinhibitorinhibit

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