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| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Anaerobic microorganisms are affected by metronidazole hydrochloride in the following ways: (a) through cell membrane crossing; (b) through reductive action; (c) through interaction with intracellular targets; and (d) through the release of inactive end products that interact with hazardous nitro and sub-nitro derivatives [1]. The anaerobic protozoa Trichomonas vaginalis, Entamoeba histolytica, Giardia, and Escherichia coli are all inhibited by metronidazole hydrochloride [1]. With its good bactericidal activity, metronidazole hydrochloride (4~8 μg/mL) can suppress anaerobic bacteria [1]. Inducing Blastocystis granule formation and apoptosis, metronidazole hydrochloride (0.1 μg/mL-0.01 mg/mL; 12-96 hours) is the method used [2].
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| ln Vivo |
After being administered to rats for an extended period of time, metronidazole hydrochloride (135 mg/kg/d; po; 28 d) can cross the blood-brain barrier and cause neurotoxicity [3]. Oral metronidazole hydrochloride (1 g/L) administered for four weeks results in atrophy of the skeletal muscle and changes the expression of genes related to peripheral circadian mechanisms and muscle metabolism [4].
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| Cell Assay |
Apoptosis analysis [2]
Cell Types: Blastocystis sp. Cell Tested Concentrations: 0.1 μg/mL-0.01 mg/mL Incubation Duration: 12, 24, 48, 60, 72, 84, 96 hrs (hours) Experimental Results: The cell diameter diminished, which It is a sign of apoptotic cells and causes cells to shrink. |
| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rat (200-220 g) [3]
Doses: 135 mg/kg Route of Administration: po (oral gavage); one time/day; 28-day Experimental Results: Caused an increase in inflammatory markers, including iNOS , eNOS, Bax and caspase 3 protein expression increased, causing oxidative stress damage to brain tissue and increased MDA content. Animal/Disease Models: SPF C57Bl/6J mice (6-7 months old) [4] Doses: 1 g/L (full dose) Route of Administration: po (oral gavage); provide drinking water for 4 weeks, changed twice a week. Experimental Results: Resulting in increased expression of muscle core clock and effector genes Cry2, Ror-β, E4BP4, PP ARγ and adiponectin. Hind limb muscle weight is diminished, resulting in smaller tibialis anterior muscle fibers. |
| References |
[1]. Scully BE. Metronidazole. Med Clin North Am. 1988 May;72(3):613-21.
[2]. Dhurga DB, et al. Granular Formation during Apoptosis in Blastocystis sp. Exposed to Metronidazole (MTZ). PLoS One. 2016 Jul 29;11(7):e0155390. [3]. Chaturvedi S, et al. Mechanistic exploration of quercetin against metronidazole induced neurotoxicity in rats: Possible role of nitric oxide isoforms and inflammatory cytokines. Neurotoxicology. 2020 Jul;79:1-10. [4]. Manickam R, et al. Metronidazole Causes Skeletal Muscle Atrophy and Modulates Muscle Chronometabolism. Int J Mol Sci. 2018 Aug 16;19(8):2418. |
| Molecular Formula |
C6H10CLN3O3
|
|---|---|
| Molecular Weight |
207.614900112152
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| CAS # |
69198-10-3
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| Related CAS # |
Metronidazole;443-48-1;Metronidazole-d4 hydrochloride;1261397-74-3
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| SMILES |
Cl.OCCN1C(C)=NC=C1[N+]([O-])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8167 mL | 24.0836 mL | 48.1672 mL | |
| 5 mM | 0.9633 mL | 4.8167 mL | 9.6334 mL | |
| 10 mM | 0.4817 mL | 2.4084 mL | 4.8167 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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