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Benznidazole Parasite inhibitor

Name: Benznidazole
Brand: Selleck Chemicals
SKU: S3741
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S3741

Benznidazole (Radanil) is a nitroimidazole derivative having an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.

Chemical Structure

Molecular Weight: 260.25

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Quality Control

Batch: Purity: 99.87%

99.87

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Reverse Transcriptase HIV HCV Protease
Other Parasite Products	Diminazene Aceturate Oxibendazole Arteether Diclazuril Oxfendazole Fenbendazole α-santonin Nicarbazin Pyrantel Pamoate Carica Papaya Fruit Extract

Solubility

In vitro
Batch:

DMSO : 52 mg/mL (199.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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 ddH₂O, 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.

Chemical Information, Storage & Stability

Molecular Weight	260.25	Formula	C₁₂H₁₂N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	22994-85-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Radanil			Smiles	C1=CC=C(C=C1)CNC(=O)CN2C=CN=C2[N+](=O)[O-]

Mechanism of Action

In vitro	Benznidazole (BZL) inhibits the proliferation of leukemic non-adherent cells by controlling cell cycle at G0/G1 cell phase through up-regulation of p27. Growth inhibition induced by this compound is a reversible process, not accompanied by significant cell death. Besides its trypanocidal activity, it also has an immunomodulatory effect on macrophages by blocking the transcription of some pro-inflammatory mediators without altering interleukin 10 expression.
In vivo	In mice, oral administration of Benznidazole (100 mg/kg): the time to reach maximum concentration (Tmax) in plasma was 0.83 h, and the maximum concentration (Cmax) in plasma was 41.61 μg/ml. The elimination half-life (t_1/2b) of this compound was 2.03 h, and mean residence time (MRT) was 3.86 h. The volume of distribution (V) and clearance (CL), both as a function of its bioavailability (F), were 38.81 ml and 13.29 ml/h, respectively. In Wistar rats treated orally, T_maxs of this chemical are 2.0 and 1.1 h, respectively. Tmaxs of 15, 30, or 60 min, depending on the dose, in BALB/c mice following intraperitoneal treatment and Tmaxs of 1 to 5 h for dogs treated orally. It can cross the blood-brain barrier and exert its action in cases of central nervous system parasitism. However, other studies have indicated that this compound has toxic effects in the central nervous system. Dogs orally treated with it presented encephalopathy with multifocal characteristics and clinical, pathological, and neurological disorders that were dose dependent and time dependent. Its biodistribution occurs broadly, reaching the heart and colon, which are the most relevant organs for T. cruzi infection, and also the spleen, brain, liver, lungs, and kidneys.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23855487/ [2] https://pubmed.ncbi.nlm.nih.gov/28167558/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03892213	Completed	Chagas Disease	Drugs for Neglected Diseases\|PhinC Development	October 2014	Phase 1
NCT01755403	Completed	Chagas Disease	Barcelona Centre for International Health Research	December 2012	Phase 4
NCT01547533	Completed	Chagas Disease\|Lactation	Hospital de Niños R. Gutierrez de Buenos Aires	August 2011	--
NCT01489228	Unknown status	Chronic Chagas Disease Indeterminate	Drugs for Neglected Diseases\|Eisai Co. Ltd.	June 2011	Phase 2
NCT00699387	Completed	Chagas Disease	Hospital de Niños R. Gutierrez de Buenos Aires\|Thrasher Research Fund\|The Hospital for Sick Children\|Fundacion Bunge y Born (Argentina)\|Universidad Nacional de La Plata\|Consejo de Investigacion en Salud Gobierno de Buenos Aires	April 2007	Not Applicable

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