Fexinidazole (Synonyms: HOE 239)

Name: Fexinidazole
Brand: MedChemExpress
SKU: HY-13801
Rating: 5.0 (4 reviews)

製品番号: HY-13801 純度: 99.84%: Data Sheet SDS COA 取扱説明書
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Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.

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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。

Fexinidazole 構造式

CAS 番号 : 59729-37-2

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 93	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 93	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$85	在庫あり	Estimated Time of Arrival: December 31
10 mg	$135	在庫あり	Estimated Time of Arrival: December 31
25 mg	$250	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.

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Fexinidazole:

Fexinidazole (Standard) お問い合わせ

顧客検証

Parasite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
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

製品説明

IC₅₀ & Target

Trypanosoma

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29885575]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30092366]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30655943]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32292551]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32652409]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32795774]
L6	IC₅₀	>90 μg/mL Compound: Fexinidazole	Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay	[PMID: 21353728]
L6	IC₅₀	377 μM Compound: 7a, fexinidazole	Cytotoxicity against rat L6 cells after 72 hrs by SRB assay Cytotoxicity against rat L6 cells after 72 hrs by SRB assay	[PMID: 21211967]
THP-1	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32652409]
THP-1	CC₅₀	>62.5 μM Compound: Fexinidazole	Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29885575]
THP-1	CC₅₀	>62.5 μM Compound: Fexinidazole	Cytotoxicity against human THP1 cells after 72 hrs by MTT assay Cytotoxicity against human THP1 cells after 72 hrs by MTT assay	[PMID: 30655943]
THP-1	CC₅₀	3.6 μM Compound: Fexinidazole	Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30092366]
THP-1	EC₅₀	2.8 μM Compound: D	Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as decrease infected macrophages after 120 hrs by microscopy Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as decrease infected macrophages after 120 hrs by microscopy	[PMID: 25846065]
Vero	EC₅₀	3 μM Compound: Fexinidazole	Antitrypanosomal activity against Trypanosoma cruzi CL Brener amastigotes infected in African green monkey Vero cells assessed as reduction in parasite growth incubated for 120 hrs at 24 hrs post-infection and measured on day 6 post-infection by hemocytom Antitrypanosomal activity against Trypanosoma cruzi CL Brener amastigotes infected in African green monkey Vero cells assessed as reduction in parasite growth incubated for 120 hrs at 24 hrs post-infection and measured on day 6 post-infection by hemocytom	[PMID: 32292551]

体外実験

Fexinidazole (HOE 239) has two principal metabolites, sulfoxide and sulfone. They have shown trypanocidal activity in vitro with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml) range against all parasite strains tested^[1].

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

体内実験

Fexinidazole (HOE 239; 20-50 mg/kg/day of IP or 25-100 mg/kg/day of PO; four consecutive days) has antitrypanosomal activities^[1].

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

Animal Model:	Adult female NMRI mice weighing between 20 and 25 g T. b. rhodesiense^[1]
Dosage:	20, 50 mg/kg (IP) or 25, 50, 100 mg/kg (PO)
Administration:	IP or PO; daily; four consecutive days
Result:	Had antitrypanosomal activities, with 100 mg/kg/day p.o. being 100% curative.

臨床実験

分子量

279.31

分子式

C₁₂H₁₃N₃O₃S

CAS 番号

59729-37-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=[N+](C1=CN=C(COC2=CC=C(SC)C=C2)N1C)[O-]

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 : 50 mg/mL (179.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5803 mL	17.9013 mL	35.8025 mL
5 mM	0.7161 mL	3.5803 mL	7.1605 mL
10 mM	0.3580 mL	1.7901 mL	3.5803 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 (8.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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% Corn Oil
Solubility: 2.5 mg/mL (8.95 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.5 mg/mL. 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: 99.92%

Select Batch:

データシート (273 KB) SDS (393 KB)

COA (247 KB) HNMR (173 KB) RP-HPLC (225 KB) LCMS (476 KB) Elemental Analysis Report (105 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Kaiser M, et al. Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness. Antimicrob Agents Chemother. 2011 Dec;55(12):5602-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5803 mL	17.9013 mL	35.8025 mL	89.5063 mL
	5 mM	0.7161 mL	3.5803 mL	7.1605 mL	17.9013 mL
	10 mM	0.3580 mL	1.7901 mL	3.5803 mL	8.9506 mL
	15 mM	0.2387 mL	1.1934 mL	2.3868 mL	5.9671 mL
	20 mM	0.1790 mL	0.8951 mL	1.7901 mL	4.4753 mL
	25 mM	0.1432 mL	0.7161 mL	1.4321 mL	3.5803 mL
	30 mM	0.1193 mL	0.5967 mL	1.1934 mL	2.9835 mL
	40 mM	0.0895 mL	0.4475 mL	0.8951 mL	2.2377 mL
	50 mM	0.0716 mL	0.3580 mL	0.7161 mL	1.7901 mL
	60 mM	0.0597 mL	0.2984 mL	0.5967 mL	1.4918 mL
	80 mM	0.0448 mL	0.2238 mL	0.4475 mL	1.1188 mL
	100 mM	0.0358 mL	0.1790 mL	0.3580 mL	0.8951 mL

Fexinidazole 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:

Fexinidazole59729-37-2HOE 239HOE239HOE-239ParasiteorallynitroimidazoleantitrypanosomalT.bruceisleepingsicknessHATInhibitorinhibitorinhibit

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Fexinidazole (Synonyms: HOE 239)

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Fexinidazole Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Fexinidazole (Synonyms: HOE 239)

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Other Forms of Fexinidazole:

Fexinidazole 関連抗体

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•関連スクリーニングライブラリ:

•関連小分子:

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生物活性

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

Fexinidazole 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Fexinidazole Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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