| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| 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].
|
| 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. |
| Additional Infomation |
Metronidazole hydrochloride is a hydrochloride salt composed of equimolar amounts of metronidazole and hydrogen chloride. It possesses a variety of pharmacological activities, including antibacterial, antimicrobial, antiparasitic, antitrichomonal, prodrug, and antiamoebic activities. It contains metronidazole(1+) ions. Metronidazole hydrochloride is a hydrochloride salt of synthetic nitroimidazole derivatives, exhibiting antiprotozoal and antibacterial activities. Although its mechanism of action is not fully elucidated, unionized metronidazole is readily absorbed by obligate anaerobes and subsequently reduced to the active intermediate by electron transport proteins with low redox potentials. Reduced metronidazole can cause DNA strand breaks, thereby inhibiting DNA synthesis and bacterial cell growth. It is a nitroimidazole drug used to treat amebiasis, vaginitis, trichomoniasis, and giardiasis. It is also effective against anaerobes and spirochetes. See also: Metronidazole (with the active moiety).
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| Molecular Formula |
C6H10CLN3O3
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|---|---|
| Molecular Weight |
207.614900112152
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| Exact Mass |
207.041
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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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| PubChem CID |
68592
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| Appearance |
Oil
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| Boiling Point |
405.4ºC at 760 mmHg
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| Melting Point |
158-160ºC
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| Flash Point |
199ºC
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| LogP |
1.417
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
|
| Heavy Atom Count |
13
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| Complexity |
170
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=NC=C(N1CCO)[N+](=O)[O-].Cl
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| InChi Key |
FPTPAIQTXYFGJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H9N3O3.ClH/c1-5-7-4-6(9(11)12)8(5)2-3-10;/h4,10H,2-3H2,1H3;1H
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| Chemical Name |
2-(2-methyl-5-nitroimidazol-1-yl)ethanol;hydrochloride
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| HS Tariff Code |
2934.99.9001
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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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~481.7 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (12.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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