BTZ043
Based on 4 publication(s) in Google Scholar
BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 1161233-85-7
- Formula: C17H16F3N3O5S
- Molecular Weight:431.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BTZ043
MoreAll Antibiotic Isoforms
More
Biological Activity
DprE1[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | CC50 |
58 μM
Compound: 29; BTZ043
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Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
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[PMID: 35612311] |
| HEK293 | CC50 |
>10 μM
Compound: 2, BTZ-10526043, BTZ043
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Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay
Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay
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[PMID: 22916795] |
| HeLa | CC50 |
>1.2 x 102μM
Compound: 1; BTZ-043
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Cytotoxicity against human HeLa cells assessed as cytolytic effect incubated for 72 hrs by methylene blue staining based colorimetric analysis
Cytotoxicity against human HeLa cells assessed as cytolytic effect incubated for 72 hrs by methylene blue staining based colorimetric analysis
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[PMID: 38071794] |
| HeLa | CC50 |
>20 μM
Compound: 1, BTZ043
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Cytotoxicity against human HeLa cells after 72 hrs by crystal violet biomass reduction assay
Cytotoxicity against human HeLa cells after 72 hrs by crystal violet biomass reduction assay
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[PMID: 25699139] |
| HeLa | CC50 |
>50 μM
Compound: 2, BTZ-10526043, BTZ043
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Cytotoxicity against human HeLa cells after 72 hrs by methylene blue staining
Cytotoxicity against human HeLa cells after 72 hrs by methylene blue staining
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[PMID: 22916795] |
| HepG2 | CC50 |
>10 μM
Compound: 2, BTZ-10526043, BTZ043
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Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
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[PMID: 22916795] |
| HUVEC | GI50 |
8 μM
Compound: 2, BTZ-10526043, BTZ043
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Antiproliferative activity against human HUVEC cells after 72 hrs by methylene blue staining
Antiproliferative activity against human HUVEC cells after 72 hrs by methylene blue staining
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[PMID: 22916795] |
| K562 | GI50 |
11 μM
Compound: 2, BTZ-10526043, BTZ043
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Antiproliferative activity against human K562 cells after 72 hrs by electronic cell analysis
Antiproliferative activity against human K562 cells after 72 hrs by electronic cell analysis
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[PMID: 22916795] |
| MCF7 | CC50 |
>20 μM
Compound: 1, BTZ043
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Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet biomass reduction assay
Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet biomass reduction assay
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[PMID: 25699139] |
| PC-3 | CC50 |
>20 μM
Compound: 1, BTZ043
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Cytotoxicity against human PC3 cells after 72 hrs by crystal violet biomass reduction assay
Cytotoxicity against human PC3 cells after 72 hrs by crystal violet biomass reduction assay
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[PMID: 25699139] |
| Vero | IC50 |
>100 μM
Compound: 5; BTZ043
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Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay
Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay
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[PMID: 34046598] |
| Vero | IC50 |
>64 μg/mL
Compound: 1; BTZ043
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 30336450] |
The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis are 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively[2]. The in vitro activity of BTZ043 against 30 Nocardia brasiliensis isolates is also tested. The MIC50 and MIC90 values for BTZ043 are 0.125 and 0.25 μg/mL. The MIC for N. carnea ATCC 6847 is 0.003μg/mL, for N. transvalensis ATCC 6865 is 0.003μg/mL, for N. brasiliensis NCTC10300 is 0.03 μg/mL, and for N. brasiliensis HUJEG-1 is 0.125μg/mL. The MIC value for M. tuberculosis H37Rv is 0.000976 μg/mL. The MIC value of BTZ-043 is >64 μg/mL for Escherichia coli ATCC 25922 and S. aureus ATCC 29213[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1161233-85-7
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Appearance Solid
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Molecular Weight 431.39
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Formula C17H16F3N3O5S
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Color Light yellow to yellow
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SMILES
O=C1N=C(N(CC2)CCC32OC[C@H](C)O3)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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ACS Nano
2023 May 23;17(10):9478-9486. PMID: 37160267 -
J Med Chem
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors. [Abstract]2020 May 28;63(10):5367-5386. PMID: 32342688 -
ACS Pharmacol Transl Sci
A Comparative Pharmacokinetics Study of Orally and Intranasally Administered 8-Nitro-1,3-benzothiazin-4-one (BTZ043) Amorphous Drug Nanoparticles. [Abstract]2024 Nov 9;7(12):4123-4134. PMID: 39698258 -
Solvent & Solubility
DMSO : 13.3 mg/mL (30.83 mM; Need ultrasonic and warming; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.80 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.80 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mice[2]
Animal efficacy is determined in a standard mouse infection model. BALB/c mice are infected with a low bacillary load (~200 CFU) of M. tuberculosis H37Rv via aerosol. Treatment started four-weeks post infection. Mice are dosed by gavage with 37.5, or 300 mg of BTZ043, per kg body weight, in carboxymethyl cellulose formulation (0.25%), once daily, six times/week, for four weeks. Control and treated mice are sacrificed, lungs and spleens homogenized and dilutions plated for enumeration of viable bacilli[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Vadim Makarov et al. The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 fromMycobacterium tuberculosis. Antimicrob Agents Chemother, 2015 Aug, 59(8): 4446-4452. [Content Brief]
[2]. Makarov V, et al. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science. 2009 May 8;324(5928):801-4. [Content Brief]
[3]. Norma Alejandra González-Martínez et al. In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLoS Negl Trop Dis, 2015 Oct, 9(10): e0004022. [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 | 2.3181 mL | 11.5904 mL | 23.1809 mL | 57.9522 mL |
| 5 mM | 0.4636 mL | 2.3181 mL | 4.6362 mL | 11.5904 mL | |
| 10 mM | 0.2318 mL | 1.1590 mL | 2.3181 mL | 5.7952 mL | |
| 15 mM | 0.1545 mL | 0.7727 mL | 1.5454 mL | 3.8635 mL | |
| 20 mM | 0.1159 mL | 0.5795 mL | 1.1590 mL | 2.8976 mL | |
| 25 mM | 0.0927 mL | 0.4636 mL | 0.9272 mL | 2.3181 mL | |
| 30 mM | 0.0773 mL | 0.3863 mL | 0.7727 mL | 1.9317 mL |
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