| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Morinidazole is a prodrug that is converted to its active form by the action of nitroreductases in anaerobic bacteria. The active form damages bacterial DNA by causing strand breakage, leading to cell death.
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| ln Vitro |
N+-glucuronidation is one method of metabolizing morpholinidazole, leading to the N+-glucuronides of S-morpholinidazole [M8-1] and R-morpholinidazole [M8-2]. Sulfation is another method of metabolizing morpholinidazole, leading to the sulfate conjugate of morpholinidazole [M7]. M7 is a substrate of OAT1, M8-1 and M8-2 are substrates of OAT3, and Km 28.6 and 54.0 μM, respectively, are substrates of OAT1 and OAT3, respectively [1]. With minimum inhibitory concentrations (MIC) of 2 μg/mL and 3 μg/mL, respectively, morlinidazole demonstrates efficacy against Trichomonas vaginalis and Entamoeba histolytica in vitro [2].
In vitro, Morinidazole demonstrates antibacterial activity against anaerobic bacteria. Its activity is assessed by determining the minimum inhibitory concentration (MIC) against various bacterial strains. |
| ln Vivo |
Morlinidazole (20 mg/kg or 25 mg/kg; oral; single dose) has an EC50 of 20 mg/kg for Trichomonas vaginalis and 25 mg/kg for Entamoeba histolytica in rats, respectively [ 2]. Following intravenous injection, the tissues revealed varying amounts of metronidazole (50 mg/kg; 0.25, 0.75, 1.5 h); the concentrations in the mouse liver, kidney, and plasma were higher than those in the lung, heart, and spleen [ 3]. Morpholinidazole's pharmacokinetic characteristics in both control and 5/6 nephrectomized (Nx) rats [3] Collective Cmax (μg/mL) Tmax (hour) T1/2 (hour) AUC0-t (μg· h/mL) AUC0-∞ (μg) ·h/mL) CL (mL/h/kg) Vss = mL/kg MRT in hours 48.2 0.08 1.16 87.2 87.3 582 805 control rat 53.2 0.08 1.32 91.2 91.3 552 891 1.62 1.39 5/6 Nx rat Intravenous injection; morpholinidazole at a dose of 50 mg/kg; before to dosing (0 hours); 5, 15, and 30 minutes following dosage; along with 1, 2, 4, 6, and At eight and twelve hours, blood samples were taken from the retroorbital venous plexus.
In vivo, Morinidazole is orally active and undergoes extensive metabolism in humans via N+-glucuronidation and sulfation. It is used in clinical studies for the treatment of anaerobic infections. |
| Enzyme Assay |
The assay for antibacterial activity is the broth microdilution method. Bacteria are cultured in a liquid medium in a 96-well plate. Various concentrations of Morinidazole are added, and the plate is incubated under anaerobic conditions. The minimum inhibitory concentration (MIC) is determined as the lowest concentration that inhibits visible growth.
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| Cell Assay |
Cells (bacteria) are cultured in appropriate anaerobic media. The compound is added at various concentrations, and growth inhibition is assessed by measuring optical density. The MIC is determined after a defined incubation period.
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| Animal Protocol |
Animal/Disease Models: SD rat renal failure model (180-220 g) [3]
Doses: 50 mg/kg Route of Administration: intravenous (iv) (iv)injection; rats were sacrificed at 0.25, 0.75 and 1.50 hrs (hrs (hours)) after administration Experimental Results: compared with control , plasma exposure was slightly increased. In vivo, Morinidazole is administered orally. Its efficacy is assessed in animal models of intra-abdominal infection or in clinical trials for appendicitis and PID. |
| ADME/Pharmacokinetics |
Morinidazole has a molecular weight of 270.28 g/mol and a molecular formula of C11H18N4O4. It is an orally active compound.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Morinidazole is not detailed in the search results. As a nitroimidazole, it shares a class effect of potential genotoxicity, and its safety profile is established through clinical use.
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| References |
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| Additional Infomation |
Molinidazole is an organic molecular entity. Molinidazole is currently being investigated in the clinical trial NCT03380793 (a trial evaluating the efficacy and safety of Molinidazole in patients with appendicitis).
Morinidazole is a research compound and a clinically used drug in some regions for the treatment of anaerobic bacterial infections. It is an example of a nitroimidazole antibiotic used for its broad-spectrum activity against anaerobes. |
| Molecular Formula |
C11H18N4O4
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|---|---|
| Molecular Weight |
270.285022258759
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| Exact Mass |
270.132
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| CAS # |
92478-27-8
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| Related CAS # |
(R)-Morinidazole;898230-59-6
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| PubChem CID |
11644726
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
521.4±50.0 °C at 760 mmHg
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| Flash Point |
269.2±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
0.46
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
306
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GAZGHCHCYRSPIV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H18N4O4/c1-9-12-6-11(15(17)18)14(9)8-10(16)7-13-2-4-19-5-3-13/h6,10,16H,2-5,7-8H2,1H3
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| Chemical Name |
1-(2-methyl-5-nitroimidazol-1-yl)-3-morpholin-4-ylpropan-2-ol
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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)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~369.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (10.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.75 mg/mL (10.17 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 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (10.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6997 mL | 18.4986 mL | 36.9973 mL | |
| 5 mM | 0.7399 mL | 3.6997 mL | 7.3995 mL | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6997 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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