Home Microbiology Parasite inhibitor Benznidazole For research use only.

Benznidazole

Synonyms: Radanil

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

Benznidazole Chemical Structure

Benznidazole Chemical Structure

CAS No. 22994-85-0

Purity & Quality Control

Benznidazole Related Products

Biological Activity

Description Benznidazole (Radanil) is a nitroimidazole derivative having an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.
In vitro
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 BZL is a reversible process, not accompanied by significant cell death. Besides its trypanocidal activity, BZL also has an immunomodulatory effect on macrophages by blocking the transcription of some pro-inflammatory mediators without altering interleukin 10 expression[1].
Cell Research Cell lines THP-1 cells
Concentrations 0.1, 0.5 or 1 mM
Incubation Time 24 or 48 h
Method

20000 cells in 200 mL of complete medium were incubated in quadruplicate in a 96-well plate in the presence of BZL (0.1, 0.5 and 1 mM) or vehicle (0.1% DMSO) for 24 or 48 h and then 20 mL of MTT solution (5 mg/mL in phosphate-buffered saline [PBS]) was added to each well. After 2 h at 37 ℃, the MTT solution was removed and precipitated formazan was solubilized in 200 mL DMSO. Formazan production was then measured at OD545nm in a micro plate spectrophotometer, with DMSO as blank.
In Vivo
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 (t1/2b) of Benznidazole 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 Benznidazole bioavailability (F), were 38.81 ml and 13.29 ml/h, respectively. In Wistar rats treated orally, Tmaxs of Benznidazole 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. Benznidazole can cross the blood-brain barrier and exert its action in cases of central nervous system parasitism. However, other studies have indicated that BNZ has toxic effects in the central nervous system. Dogs orally treated with BNZ presented encephalopathy with multifocal characteristics and clinical, pathological, and neurological disorders that were dose dependent and time dependent. Benznidazole 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[2].
Animal Research Animal Models Swiss mice 
Dosages 100 mg/kg
Administration by gavage
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

Chemical Information & Solubility

Molecular Weight 260.25 Formula

C12H12N4O3
CAS No. 22994-85-0 SDF Download Benznidazole SDF
Smiles C1=CC=C(C=C1)CNC(=O)CN2C=CN=C2[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 52 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Benznidazole | Benznidazole ic50 | Benznidazole price | Benznidazole cost | Benznidazole solubility dmso | Benznidazole purchase | Benznidazole manufacturer | Benznidazole research buy | Benznidazole order | Benznidazole mouse | Benznidazole chemical structure | Benznidazole mw | Benznidazole molecular weight | Benznidazole datasheet | Benznidazole supplier | Benznidazole in vitro | Benznidazole cell line | Benznidazole concentration | Benznidazole nmr