Metronidazole Antineoplastic and Immunosuppressive Antibiotics inhibitor

Cat.No.S1907

Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa.
Metronidazole  Antineoplastic and Immunosuppressive Antibiotics inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 171.15

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 171.15 Formula

C6H9N3O3

Storage (From the date of receipt)
CAS No. 443-48-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=NC=C(N1CCO)[N+](=O)[O-]

Solubility

In vitro
Batch:

DMSO : 34 mg/mL (198.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 12 mg/mL (Warmed with 50℃ water bath; Ultrasonicated)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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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.

Mechanism of Action

Targets/IC50/Ki
DNA synthesis [1]
In vitro
Metronidazole is relatively inactive until it is metabolized within host or microbial cells. It is activated when it receives an electron from ferredoxin or flavodoxin that is reduced by POR in anaerobic or microaerophilic bacteria or luminal parasites. This compound damages cells by forming protein and DNA adducts. [1] It has activity against protozoans like Entamoeba histolytica, Giardia lamblia and Trichomonas vaginalis, for which the drug is first approved as an effective treatment. The activity of this chemical against anaerobic bowel flora has been used for prophylaxis and treatment of patients with Crohn's disease who might develop an infectious complication. It has played an important role in anaerobic-related infections. This compound has notable effectiveness in treating anaerobic brain abscesses. [2] Its resistance tends to result from de novo mutation in the resident rdxA gene, rather than from lateral transfer of mutant rdxA (or other) genes from unrelated but Mtzr strains. It partially inhibits growth stimulate forward mutation to rifampin resistance in rdxA(+) (Metronidazole(s)) and also in rdxA (Metronidazole(r)) H. pylori strains, and that expression of rdxA in Escherichia coli results in equivalent Mtz-induced mutation. [3] This compound leads to apoptosis-like features in growing cultures of axenic B. hominis, including key morphological and biochemical features of programmed cell death (PCD), viz. nuclear condensation and nicked DNA in nucleus, reduced cytoplasmic volume, externalization of phosphatidylserine and maintenance of plasma membrane integrity with increasing permeability. [4]
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06387147 Not yet recruiting
Acute Mesenteric Ischemia
Assistance Publique - Hôpitaux de Paris
September 1 2024 Phase 3
NCT05748145 Recruiting
Colorectal Cancer
Oncology Institute of Southern Switzerland
September 11 2023 Phase 2
NCT04273997 Unknown status
Pilonidal Sinus
S.L.A. Pharma AG
October 1 2021 Phase 2

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