| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| ln Vitro |
(R)-morpholinidazole is metabolized by N+-glucuronidation, which results in the sulfate conjugate of (R) to the N+-glucuronide of the S-morpholinidazole R enantiomer [M8-1] and the N+-glucuronide of (R)-morpholinidazole [M8-2], which is sulfated to yield morpholinidazole [M7][1]. M7 serves as a substrate for 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]. In vitro, (R)-Morlinidazole demonstrates efficacy against Trichomonas vaginalis and Entamoeba histolytica, with minimum inhibitory concentrations (MIC) of 2 μg/mL and 3 μg/mL, respectively [2].
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| ln Vivo |
(R)-Morlinidazole (20 mg/kg or 25 mg/kg; oral; single dosage) suppresses Entamoeba histolytica and Trichomonas vaginalis in rats, with EC50 values of 20 mg/kg and 25, respectively, mg/kg[2]. Following an intravenous injection, the concentrations of (R)-morlinidazole (50 mg/kg; 0.25, 0.75, 1.5 h) varied in the tissues. The amounts in the kidney, liver, and plasma of mice were greater than those in the lung and lung. Spleen and Heart. 3]. The pharmacokinetic parameters of (R)-morpholinidazole were studied in both control and 5/6 nephrectomized (Nx) rats [3]. gang Cmax in micrograms per milliliter Maximum Time (h) T1/2(h) AUC0-t (μg^h/mL) (μg·h/mL) AUC0 -∞ CL (milliliters/hour/kg) Vss (mL/kg) MRT (hours) Rat control 48.2 0.08 1.16 87.2 87.3 582 805 1.39 5/6 Nx Rat 53.2 0.08 1.32 91.2 91.3 552 891 1.62 50 mg/kg (R)-Morlinidazole was administered intravenously. Blood samples were taken from the retroorbital venous plexus before the dose (0 hours), 5, 15, and 30 minutes after the dose, and 1 after the dose, 2, 4, 6, 8, and 12 hours.
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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. |
| References |
[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.
[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. [3]. Lu Aifeng, et al. Application of α-(morpholine-1-yl)methyl-2-methyl-nitroimidazole-1-ethanol as anti-trichomonal agent and amebacide: China, CN1981764[P]. 2007-06-20. |
| Molecular Formula |
C11H18N4O4
|
|---|---|
| Molecular Weight |
270.285022258759
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| Exact Mass |
270.132
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| CAS # |
898230-59-6
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| Related CAS # |
Morinidazole;92478-27-8
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| PubChem CID |
92044393
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| Appearance |
Typically exists as solid at room temperature
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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 |
1
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| SMILES |
C(N1C(C)=NC=C1[N+](=O)[O-])[C@H](O)CN1CCOCC1
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| InChi Key |
GAZGHCHCYRSPIV-SNVBAGLBSA-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/t10-/m1/s1
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| Chemical Name |
(2R)-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: ≥ 2.5 mg/mL (9.25 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 25.0 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: ≥ 2.5 mg/mL (9.25 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 25.0 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: ≥ 2.5 mg/mL (9.25 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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