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Morinidazole

Cat No.:V13773 Purity: ≥98%
Morinidazole was approved by China Food and Drug Administration (CFDA) on February 24, 2014.
Morinidazole
Morinidazole Chemical Structure CAS No.: 92478-27-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
1g
Other Sizes

Other Forms of Morinidazole:

  • Morinidazole R enantiomer
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Morinidazole was approved by China Food and Drug Administration (CFDA) on February 24, 2014. Morinidazole is a nitroimidazoles antibiotic used to treat bacterial infections including appendicitis and pelvic inflammatory disease. Morinidazole is a nitroimidazoles antibiotic indicated for the treatment of bacterial infections including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.

Biological Activity I Assay Protocols (From Reference)
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].
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.
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]. 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]. 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]. Application of α-(morpholine-1-yl)methyl-2-methyl-nitroimidazole-1-ethanol as anti-trichomonal agent and amebacide: China, CN1981764[P]. 2007-06-20.

Additional Infomation
Morinidazole is an organic molecular entity.
Morinidazole is under investigation in clinical trial NCT03380793 (A Trial to Assess the Efficacy and Safety of Morinidazole in Patients With Appendicitis).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H18N4O4
Molecular Weight
270.285022258759
Exact Mass
270.132
CAS #
92478-27-8
Related CAS #
(R)-Morinidazole;898230-59-6
PubChem CID
11644726
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
521.4±50.0 °C at 760 mmHg
Flash Point
269.2±30.1 °C
Vapour Pressure
0.0±1.4 mmHg at 25°C
Index of Refraction
1.632
LogP
0.46
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
4
Heavy Atom Count
19
Complexity
306
Defined Atom Stereocenter Count
0
InChi Key
GAZGHCHCYRSPIV-UHFFFAOYSA-N
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
Chemical Name
1-(2-methyl-5-nitroimidazol-1-yl)-3-morpholin-4-ylpropan-2-ol
HS Tariff Code
2934.99.9001
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 Data
Solubility (In Vitro)
DMSO : ≥ 100 mg/mL (~369.97 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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