Tinidazole Chemical Structure

Tinidazole Chemical Structure
Molecular Weight: 247.27

Validation & Quality Control

Quality Control & MSDS

Product Information

Product Description

Biological Activity

Description Tinidazole is an anti-parasitic drug.
In vitro Tinidazole kills the metronidazole-susceptible isolates at a low MLC but is effective against only 4 of the 12 metronidazole-resistant isolates. [1] Tinidazole exhibits activity against pathogenic protozoa (eg, Tricbomonas vaginalis, Entamoeba bistolytica, Giardia duodenalis), a wide range of clinically significant anaerobic bacteria (eg, Bacteroides fragilis, Clostridium difficile), and the microaerophilic bacterium Helicobacter pylori. Tinidazole is reduced to cytotoxic intermediates that covalently bind to DNA, causing irreversible damage in susceptible protozoal and bacterial cells. [2] Tinidazole inhibits against 104 T. vaginalis isolates with mean MLC of 1014.9 μM. [3] Tinidazole slightly affects trophozoite morphology, adherence and viability against Giardia duodenalis. [4] Tinidazole is against 40 Clostridium difficile, 10 Prevotella bivia and 11 Bacteroides fragilis clinical isolates, the geometric mean MICs of tinidazole and metronidazole are, respectively: C. difficile, 0.31 μg/mL and 0.28 μg/mL; P. bivia, 2.33 μg/mL and 1.52 μg/mL; B. fragilis, 0.5 μg/mL and 0.71 μg/mL. [5]
In vivo
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Narcisi EM, et al. Antimicrob Agents Chemother, 1996, 40(5), 1121-1125.

[2] Fung HB, et al. Clin Ther, 2005, 27(12), 1859-1884.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01070277 Recruiting Chronic Diarrhea|Abdominal Pain|Bloating Sheba Medical Center March 2012 --
NCT01481844 Recruiting H Pylori Treatment Soroka University Medical Center November 2011 Phase 3
NCT01544517 Completed Helicobacter Pylori Infection Second University of Naples January 2011 Phase 3
NCT01591889 Completed Trichomoniasis Roxane Laboratories September 2009 Phase 1
NCT00811096 Completed Malaria, Vivax Walter Reed Army Institute of Research (WRAIR) November 2008 Phase 2

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Chemical Information

Download Tinidazole SDF
Molecular Weight (MW) 247.27
Formula

C8H13N3O4S

CAS No. 19387-91-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CP12574
Solubility (25°C) * In vitro DMSO 49 mg/mL (198.16 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1H-Imidazole, 1-[2-(ethylsulfonyl)ethyl]-2-methyl-5-nitro-

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