Art. -Nr.: HY-13579

BTZ043

Name: BTZ043
Brand: MedChemExpress
SKU: HY-13579
Price: 80.00 USD
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4 Cited Publications

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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.

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Reinheit : 99.51%
CAS. Nr.: 1161233-85-7
Formel: C₁₇H₁₆F₃N₃O₅S
Molecular Weight:431.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BTZ043 Chemical Structure

CAS. Nr.: 1161233-85-7

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target

DprE1^[1].

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	CC₅₀	58 μM Compound: 29; BTZ043	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 35612311]
HEK293	CC₅₀	>10 μM Compound: 2, BTZ-10526043, BTZ043	Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay	[PMID: 22916795]
HeLa	CC₅₀	>1.2 x 10²μM Compound: 1; BTZ-043	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	[PMID: 38071794]
HeLa	CC₅₀	>20 μM Compound: 1, BTZ043	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	[PMID: 25699139]
HeLa	CC₅₀	>50 μM Compound: 2, BTZ-10526043, BTZ043	Cytotoxicity against human HeLa cells after 72 hrs by methylene blue staining Cytotoxicity against human HeLa cells after 72 hrs by methylene blue staining	[PMID: 22916795]
HepG2	CC₅₀	>10 μM Compound: 2, BTZ-10526043, BTZ043	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 22916795]
HUVEC	GI₅₀	8 μM Compound: 2, BTZ-10526043, BTZ043	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	[PMID: 22916795]
K562	GI₅₀	11 μM Compound: 2, BTZ-10526043, BTZ043	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	[PMID: 22916795]
MCF7	CC₅₀	>20 μM Compound: 1, BTZ043	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	[PMID: 25699139]
PC-3	CC₅₀	>20 μM Compound: 1, BTZ043	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	[PMID: 25699139]
Vero	IC₅₀	>100 μM Compound: 5; BTZ043	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	[PMID: 34046598]
Vero	IC₅₀	>64 μg/mL Compound: 1; BTZ043	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	[PMID: 30336450]

In Vitro

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.

In Vivo

Four weeks of treatment with BTZ043 reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional results suggest that BTZ043 efficacy is time-rather than dose-dependent. Acute (5 g/kg) and chronic (25 and 250 mg/kg) toxicology studies in uninfected mice show that, even at the highest dose tested, there are no adverse anatomical, behavioral, or physiological effects after one month^[2].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1161233-85-7
Appearance Solid
Molecular Weight 431.39
Formel C₁₇H₁₆F₃N₃O₅S
Color Light yellow to yellow
SMILES

O=C1N=C(N(CC2)CCC32OC[C@H](C)O3)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

ACS Nano

Amorphous Drug Nanoparticles for Inhalation Therapy of Multidrug-Resistant Tuberculosis. [Abstract]

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
ChemNanoMat

2020 Oct 28.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3181 mL

11.5904 mL

23.1809 mL

5 mM

0.4636 mL

2.3181 mL

4.6362 mL

10 mM

0.2318 mL

1.1590 mL

2.3181 mL

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.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. 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]

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.

Complete Stock Solution Preparation Table

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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Keywords

BTZ043

4 Cited Publications

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BTZ043

Publications Citing Use of MedChemExpress (MCE) BTZ043

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