BTZ043

Name: BTZ043
Brand: MedChemExpress
SKU: HY-13579
Rating: 5.0 (4 reviews)

製品番号: HY-13579 純度: 99.51%: Data Sheet SDS COA 取扱説明書
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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

BTZ043 構造式

CAS 番号 : 1161233-85-7

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$80	在庫あり	Estimated Time of Arrival: December 31
10 mg	$125	在庫あり	Estimated Time of Arrival: December 31
50 mg	$400	在庫あり	Estimated Time of Arrival: December 31
100 mg	$600	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 4 publication(s) in Google Scholar

Other Forms of BTZ043:

BTZ043 Racemate 在庫あり
BTZ043 (Standard) お問い合わせ

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すべてのアイソフォームを表示

Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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製品説明

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].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	CC₅₀	58 3 Compound: 29; BTZ043	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 35612311]
A549	CC₅₀	58 3 Compound: 29; BTZ043	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 35612311]
HEK293	CC₅₀	> 10 3 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]
HEK293	CC₅₀	>10 3 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]
HEK293	CC₅₀	> 10 3 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	> 20 3 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]
HUVEC	GI₅₀	8 3 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]
HeLa	CC₅₀	>20 3 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 3 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 3 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]
HeLa	CC₅₀	> 1.2 x 10² 3 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	>50 3 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]
HUVEC	GI₅₀	8 3 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]
HeLa	CC₅₀	> 20 3 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]
HepG2	CC₅₀	>10 3 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]
K562	GI₅₀	11 3 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]
HeLa	CC₅₀	> 50 3 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]
HUVEC	GI₅₀	8 3 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]
HepG2	CC₅₀	> 10 3 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]
K562	GI₅₀	11 3 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 3 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]
MCF7	CC₅₀	>20 3 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 3 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]
K562	GI₅₀	11 3 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]
Vero	IC₅₀	> 100 3 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]
MCF7	CC₅₀	> 20 3 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 3 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]
PC-3	CC₅₀	> 20 3 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	> 64 6 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]
Vero	IC₅₀	>64 6 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]
Vero	IC₅₀	>100 3 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	> 100 3 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 6 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]

体外実験

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.

体内実験

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.

臨床実験

分子量

431.39

分子式

C₁₇H₁₆F₃N₃O₅S

CAS 番号

1161233-85-7

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.51%

Select Batch:

データシート (279 KB) SDS (393 KB)

COA (251 KB) RP-HPLC (244 KB)

取扱説明書 (2659 KB)

参考文献

[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]

動物実験
^[2]

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) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[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

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

BTZ043 Related Classifications

Infection

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BTZ0431161233-85-7BTZ 043BTZ-043BacterialAntibiotictuberculosis,Inhibitorinhibitorinhibit

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BTZ043

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Complete Stock Solution Preparation Table

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Dilution Calculator

The molarity calculator equation

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BTZ043

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Other Forms of BTZ043:

BTZ043 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Antibiotic アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

BTZ043 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

BTZ043 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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