- TBA-7371
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- $41.00
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2026-05-11
- CAS:1494675-86-3
- Purity: 99.74%
- Supply Ability: 10g
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| Product Name: | ZA7371 | | Synonyms: | N-(2-Hydroxyethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]-6-methyl-1H-pyrrolo[3,2-b]pyridine-3-carboxamide;ZA7371;DprE1-IN-1;AZ-7371;AZ-7371(DprE1-IN-1);TBA-7371;DprE1-IN-1 ZA7371;AZ7371;AZ 7371 | | CAS: | 1494675-86-3 | | MF: | C18H21N5O3 | | MW: | 355.39 | | EINECS: | | | Product Categories: | | | Mol File: | 1494675-86-3.mol |  |
| | ZA7371 Chemical Properties |
| Boiling point | 691.6±55.0 °C(Predicted) | | density | 1.34±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 11 mg/mL (30.95 mM) | | pka | 12.79±0.46(Predicted) | | form | A crystalline solid | | color | White to off-white |
| | ZA7371 Usage And Synthesis |
| Uses | 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]. | | 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]. | 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. |
| | References | [1] Gawad J, et al. Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1): challenging target for antitubercular drug discovery. Chem Cent J. 2018 Jun 23;12(1):72. DOI:10.1186/s13065-018-0441-2
[2] Robertson GT, et al. Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 Inhibitors TBA-7371, PBTZ169, and OPC-167832. Antimicrob Agents Chemother. 2021 Oct 18;65(11):e0058321. DOI:10.1128/AAC.00583-21
[3] Li S-Y, et al. Bactericidal and sterilizing activity of novel regimens combining bedaquiline or TBAJ-587 with GSK2556286 and TBA-7371 in a mouse model of tuberculosis. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0156223. DOI:10.1128/aac.01562-23 |
| | ZA7371 Preparation Products And Raw materials |
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