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Cat. No.: HY-128866

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TBAJ-876

TBAJ-876 is an orally active diarylquinoline anti-Mycobacterium agent. TBAJ-876 regulates energy metabolism by targeting the c and ε subunits of Mycobacterium tuberculosis F-ATP synthase, exerts bactericidal activity against replicating Mycobacterium tuberculosis, and retains activity against strains carrying the Rv0678 mutation. TBAJ-876 undergoes N-demethylation in vivo to form its major active metabolite TBAJ-876-M3, which has lower lipophilicity and hERG potassium channel binding affinity. TBAJ-876 is well tolerated in BALB/c mice and significantly reduces the colony-forming units of Mycobacterium tuberculosis in the lungs. In addition, TBAJ-876 exhibits inhibitory activity against Mycobacterium abscessus, reduces bacterial loads in the lungs and spleens of infected mice, and shows no antagonistic effect when used in combination with common antibiotics. TBAJ-876 can be used in studies related to tuberculosis and Mycobacterium abscessus pulmonary diseases.

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CAS No.: 2332841-25-3
Formule: C₃₁H₃₇BrN₄O₇
Masse moléculaire:657.55

Stockage:

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

Data Sheet (280 KB)

TBAJ-876 Chemical Structure

CAS No.: 2332841-25-3

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Fluorescent Dye

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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

TBAJ-876 (0.004-0.016 mg/L) has potent in vitro bacteriostatic activity against Mycobacterium tuberculosis H37Rv (MIC 0.008-0.016 mg/L) and Mycobacterium tuberculosis Beijing VN 2002-1585 (MIC 0.004 mg/L)^[1].
TBAJ-876 (0.0001-0.016 mg/L; 10 days) shows no interaction with its metabolite M3 when tested against Mycobacterium tuberculosis Beijing VN 2002-1585^[1].
TBAJ-876 (0.00025-0.063 mg/L; 1-6 days) demonstrates time- and concentration-dependent bactericidal activity against actively replicating Mycobacterium tuberculosis H37Rv, with the highest tested concentration (0.063 mg/L) reducing bacterial load to undetectable levels by day 6^[1].
TBAJ-876 (0.00025-0.063 mg/L; up to 21 days) has limited activity against nonreplicating Mycobacterium tuberculosis H37Rv, with only the highest tested concentration (0.063 mg/L, 16× MIC) reducing bacterial load by ~1.6 log₁₀ CFU/mL over 3 weeks^[1].
TBAJ-876 (1.38-138 μM; 5 days) exerts bacteriostatic activity against M. abscessus Bamboo in vitro at concentrations of 3x, 30x, and 300x its MIC, inhibiting growth without reducing bacterial counts below the initial inoculum^[2].
TBAJ-876 (0-2 μM; 3 days) exhibits additive or synergistic in vitro interactions with commonly used anti-M. abscessus antibiotics against M. abscessus Bamboo, with no observed antagonism^[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

TBAJ-876 (1.6-25 mg/kg; oral gavage; 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.

Essai clinique

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

Chemical Information

CAS No. 2332841-25-3
Appearance Solid
Masse moléculaire 657.55
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 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)
Instruction de manipulation (2659 KB)

Références

[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

Calculateur de molarité

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

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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.

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100 mg

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