BRD-8000.3 (Synonyms: Store at -20°C) |
Catalog No.GC62876
One-Click Copy Product Info
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BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2365504-95-4
Sample solution is provided at 25 µL, 10mM.
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BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity[1]. BRD-8000.3 exhibits inhibitory activity against Mycobacterium tuberculosis (Mtb) with an MIC₉₀ value of 800nM[1]. Resistance to BRD-8000.3 could be conferred by mutations in EfpA, including substitutions V319F and A415V[2].
In vitro, BRD-8000.3 has an IC50 value greater than 50μM for HepG2[3].
In vivo, BRD-8000.3, administered orally at 150mg/kg, demonstrated good mouse plasma exposure and low risk for drug–drug interactions, prolongation of the QT interval, or hepatotoxicity[3].
References:
[1] Johnson EO, et al. Large-Scale Chemical-Genetic Strategy Enables the Design of Antimicrobial Combination Chemotherapy in Mycobacteria. ACS Infect Dis. 2020;6(1):56-63.
[2] Khandelwal NK, Gupta M, Gomez JE, et al. Structure and inhibition mechanisms of Mycobacterium tuberculosis essential transporter efflux protein A. Preprint. bioRxiv. 2024;2024.09.04.611325.
[3] Johnson EO, LaVerriere E, Office E, et al. Large-scale chemical-genetics yields new M. tuberculosis inhibitor classes. Nature. 2019;571(7763):72-78.
| Animal experiment [1]: | |
Animal models | C57BL/6 mice |
Preparation Method | Oral dosing of 12h fasted female 7-9-week-old C57BL/6 mice was performed, using 150mg/kg BRD-8000.3 in 5% (v/v) corn oil, 10% (v/v) labrasol, 5% (v/v) solutol in water. The plasma concentration of BRD-8000.3 was measured at nine time points up to 8h. |
Dosage form | 150mg/kg; p.o. |
Applications | BRD-8000.3 showed good mouse plasma exposure by oral dosing. The half-life of BRD-8000.3 in mice is 5min. |
References: | |
| Cas No. | 2365504-95-4 | SDF | |
| Synonyms | Store at -20°C | ||
| Formula | C19H21BrN4O | M.Wt | 401.3 |
| Solubility | DMSO : 50 mg/mL (124.60 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4919 mL | 12.4595 mL | 24.919 mL |
| 5 mM | 498.4 μL | 2.4919 mL | 4.9838 mL |
| 10 mM | 249.2 μL | 1.246 mL | 2.4919 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)