Morinidazole
Based on 1 publication(s) in Google Scholar
Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N+-glucuronidation and sulfation. Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
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- Pureté: 98.0%
- CAS No.: 92478-27-8
- Formule: C11H18N4O4
- Masse moléculaire:270.29
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Morinidazole
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Activité biologique
organic anion transporter[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>5000 μM
Compound: 35
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Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
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[PMID: 27643640] |
Morinidazole can be metabolized to N+-glucuronide of S-morinidazole [M8-1] and N+-glucuronide of R-morinidazole [M8-2] via N+-glucuronidation, and sulfate conjugate of morinidazole [M7] via sulfation[1].
M7 is a substrate for organic anion transporter 1 (OAT1) and OAT3 (Km=28.6 and 54.0 μM, respectively), M8-1 and M8-2 are the substrates for OAT3[1].
Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Morinidazole (50 mg/kg; i.v.; 0.25, 0.75, 1.5 h) shows a different concentration in tissues after intravenous injection, with a higher concentration in liver, kidney, plasma than lung, heart, and spleen in mice[3].
Pharmacokinetic parameters of Morinidazole in control and 5/6 nephrectomized (Nx) rats[3]
| Group | Cmax (μg/mL) | Tmax (h) | T1/2 (h) | AUC0-t (μg·h/mL) | AUC0-∞ (μg·h/mL) | CL (mL/h/kg) | Vss (mL/kg) | MRT (h) |
| Control rats | 48.2 | 0.08 | 1.16 | 87.2 | 87.3 | 582 | 805 | 1.39 |
| 5/6 Nx rats | 53.2 | 0.08 | 1.32 | 91.2 | 91.3 | 552 | 891 | 1.62 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Renal failure model in SD rats (180-220 g)[3]
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Dosage:50 mg/kg
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Administration:Intravenous injection; sacrificed rats at 0.25, 0.75, and 1.50 hours after dose administration
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Result:Increased plasma exposures slightly compared with control.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 92478-27-8
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Appearance Solid
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Masse moléculaire 270.29
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Formule C11H18N4O4
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Color White to off-white
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SMILES
OC(CN1C([N+]([O-])=O)=CN=C1C)CN2CCOCC2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : ≥ 100 mg/mL (369.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (10.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (10.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Zhong K, et al. Effects of renal impairment on the pharmacokinetics of morinidazole: uptake transporter-mediated renal clearanceof the conjugated metabolites. Antimicrob Agents Chemother. 2014 Jul;58(7):4153-61. [Content Brief]
[2]. Kong F, et al. Increased Plasma Exposures of Conjugated Metabolites of Morinidazole in Renal Failure Patients: A Critical Role of Uremic Toxins. Drug Metab Dispos. 2017 Jun;45(6):593-603. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6997 mL | 18.4986 mL | 36.9973 mL | 92.4932 mL |
| 5 mM | 0.7399 mL | 3.6997 mL | 7.3995 mL | 18.4986 mL | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6997 mL | 9.2493 mL | |
| 15 mM | 0.2466 mL | 1.2332 mL | 2.4665 mL | 6.1662 mL | |
| 20 mM | 0.1850 mL | 0.9249 mL | 1.8499 mL | 4.6247 mL | |
| 25 mM | 0.1480 mL | 0.7399 mL | 1.4799 mL | 3.6997 mL | |
| 30 mM | 0.1233 mL | 0.6166 mL | 1.2332 mL | 3.0831 mL | |
| 40 mM | 0.0925 mL | 0.4625 mL | 0.9249 mL | 2.3123 mL | |
| 50 mM | 0.0740 mL | 0.3700 mL | 0.7399 mL | 1.8499 mL | |
| 60 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5416 mL | |
| 80 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| 100 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9249 mL |
Morinidazole Related Classifications
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