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Art. -Nr.: HY-128866

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TBAJ-876

TBAJ-876 is an orally active diarylquinoline antimycobacterial agent. TBAJ-876 targets the c and ε subunits of Mycobacterium tuberculosis F-ATP synthase to modulate energy metabolism, and it exerts bactericidal activity against replicating Mycobacterium tuberculosis and retains activity against strains carrying Rv0678 mutations. TBAJ-876 undergoes N-demethylation in vivo to form the major active metabolite TBAJ-876-M3, which has lower lipophilicity and lower binding affinity for the hERG potassium channel. TBAJ-876 is well tolerated in BALB/c mice and significantly reduces the number of colony-forming units of Mycobacterium tuberculosis in the lungs. TBAJ-876 can be used in research related to tuberculosis and Mycobacterium abscessus lung disease.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2332841-25-3
Formel: C₃₁H₃₇BrN₄O₇
Molecular Weight:657.55

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Data Sheet (281 KB)

TBAJ-876 Chemical Structure

CAS. Nr.: 2332841-25-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
Vero	IC₅₀	>10 μg/mL Compound: 3; TBAJ-876	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTS-PBS assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTS-PBS assay	[PMID: 31810890]
Vero	IC₅₀	>10 μg/mL Compound: 46; TBAJ-876	Cytotoxicity against African green monkey Vero cells measured after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells measured after 72 hrs by MTT assay	[PMID: 30803745]

In Vitro

Bacterial Infection

TBAJ-876 exhibits potent in vitro inhibitory activity against Mycobacterium tuberculosis H37Rv (MIC = 0.008-0.016 mg/L) and Mycobacterium tuberculosis Beijing strain VN 2002-1585 (MIC = 0.004 mg/L)^[1].
TBAJ-876 (0.00025-0.063 mg/L; 1-6 d) exhibits time- and concentration-dependent bactericidal activity against actively replicating Mycobacterium tuberculosis H37Rv, with the highest concentration tested (0.063 mg/L) reducing the bacterial burden to undetectable levels by day 6^[1].
TBAJ-876 (0.00025-0.063 mg/L; 21 d) shows limited activity against non-replicating Mycobacterium tuberculosis H37Rv, with only the highest tested concentration (0.063 mg/L, 16× MIC) reducing the bacterial burden by approximately 1.6 log₁₀ CFU/mL within 3 weeks^[1].
TBAJ-876 (1.38-138 μM; 5 d) exhibits in vitro bacteriostatic activity against Mycobacterium abscessus Bamboo at 3×, 30×, and 300× its MIC, inhibiting bacterial growth but not reducing bacterial counts below the initial inoculum^[2].
TBAJ-876 (up to 2 μM; 3 d), when combined in vitro with commonly used anti-Mycobacterium abscessus antibiotics, exhibits additive or synergistic effects against the Mycobacterium abscessus Bamboo strain, with no antagonism observed^[2].

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

Parmacokinetics

Species	Dose	Route	AUC_0-96
Mice^[1]	1.6 mg/kg	p.o.	1.9 mg·h/L
Mice^[1]	6.3 mg/kg	p.o.	6.8 mg·h/L
Mice^[1]	25 mg/kg	p.o.	29.9 mg·h/L

In Vivo

Bacterial Infection

TBAJ-876 (1.6-25 mg/kg; i,g,; once daily, 5 days per week; 4 weeks) demonstrates dose-dependent bactericidal activity against M. tuberculosis Beijing VN 2002-1585 in BALB/c mice, with the 25 mg/kg dose reducing median lung CFU counts by 6.6 log₁₀ over 4 weeks and rendering 2/5 animals culture negative^[1].
TBAJ-876 (10-30 mg/kg; p.o.; once daily; 10 consecutive days) reduces Mycobacterium abscessus bacterial loads in the lungs and spleen of infected NOD SCID mice, with efficacy comparable to bedaquiline at the 10 mg/kg dose^[2].

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

Animal Model:

NOD.CB17-Prkdcscid/NCrCrl (NOD SCID) (8-week-old female, intranasal infection with Mycobacterium abscessus subsp. abscessus K21)^[2]
Dosage:

10 mg/kg; 30 mg/kg
Administration:

p.o.; once daily; 10 consecutive days
Result:

Achieved in vivo efficacy against M.
abscessus comparable to bedaquiline, reducing bacterial loads in the lungs and spleen relative to untreated controls at 10 mg/kg.
Demonstrated increased efficacy in reducing bacterial loads in both lungs and spleen compared to the 10 mg/kg dose at 30 mg/kg, though this difference was not statistically significant.

Related Protocols :

Bacterial live/dead nucleic-acid viability staining

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS. Nr. 2332841-25-3
Appearance Solid
Molecular Weight 657.55
Formel C₃₁H₃₇BrN₄O₇
Color White to off-white
SMILES

COC1=NC(OC)=C(OC)C([C@H](C2=CC(C=C(Br)C=C3)=C3N=C2OC)[C@@](C4=CC(OC)=NC(OC)=C4)(O)CCN(C)C)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mudde SE, et al. Relative Contributions of the Novel Diarylquinoline TBAJ-876 and its Active Metabolite to the Bactericidal Activity in a Murine Model of Tuberculosis. J Infect Dis. 2024;230(6):e1366-e1374. [Content Brief]

[2]. Sarathy JP, et al. TBAJ-876, a 3,5-Dialkoxypyridine Analogue of Bedaquiline, Is Active against Mycobacterium abscessus. Antimicrob Agents Chemother. 2020;64(4):e02404-19. Published 2020 Mar 24. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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