TBA-7371
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.61%
- CAS. Nr.: 1494675-86-3
- Formel: C18H21N5O3
- Molecular Weight:355.39
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) TBA-7371
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Biologische Aktivität
DprE1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
164.7 μM
Compound: TBA-7371
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability
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[PMID: 38232131] |
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.
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Cell Line:Mycobacterium tuberculosis Erdman
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Concentration:1 μg/mL, 10 μg/mL, 100 μg/mL
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Incubation Time:14 days
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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.
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.
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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]
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Dosage:100 mg/kg, 200 mg/kg (0.5% carboxymethylcellulose + 0.1% Tween 80)
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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)
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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.
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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]
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Dosage:50 mg/kg, 100 mg/kg, 200 mg/kg (0.5% carboxymethylcellulose + 0.1% Tween 80)
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Administration:Oral gavage, twice daily, 5 days/week for 8 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1494675-86-3
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Appearance Solid
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Molecular Weight 355.39
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Formel C18H21N5O3
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Color White to off-white
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SMILES
O=C(C1=CN(CC2=NC=NC(OC)=C2C)C3=CC(C)=CN=C31)NCCO
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis. [Abstract]2024 Feb 8;67(3):1914-1931. PMID: 38232131
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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 |
TBA-7371 Related Classifications
HY-19750 Related Classifications
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