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Benznidazole

Name: Benznidazole
Brand: Selleck Chemicals
SKU: S3741
Rating: 5 (1 reviews)

Synonyms: Radanil

Catalog No.S3741 Purity: 99.87%

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

CAS: 22994-85-0

Selleck's Benznidazole has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.87%

99.87

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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 (t_1/2b) 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, T_maxs 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

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In vivo
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In vivo Formulation Calculator

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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.

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