2. Anti-infection Neuronal Signaling
  3. Bacterial Antibiotic Monoamine Oxidase
  4. Contezolid acefosamil sodium

Contezolid acefosamil sodium  (Synonyms: MRX-4 sodium)

Cat. No.: HY-19915B Purity: 95.19%
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Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).

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Contezolid acefosamil sodium Chemical Structure

Contezolid acefosamil sodium Chemical Structure

CAS No. : 1807365-35-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Contezolid acefosamil sodium:

Contezolid acefosamil sodium Related Antibodies

Top Publications Citing Use of Products

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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MAO-A MAO-B

  • Biological Activity

  • Purity & Documentation

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Description

Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2].

IC50 & Target

Oxazolidinone

 

In Vitro

Contezolid (MRX-I) is highly potent against all Grampositive clinical isolates of staphylococci, streptococci, and enterococci, including MDR organisms such as MRSA, methicilline-resistant Streptococcus epidermidis (MRSE), penicillin-resistant Streptococci (PRSP), and VRE[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Contezolid acefosamil sodium Related Antibodies
In Vivo

Oral absorption of Contezolid (MRX-I) occurrs rapidly in mouse, rat, and dog, with peak plasma concentrations observed at 0.5−2.6 h postdose. In mouse, rat, and dog, respectively, PK parameters are determined as follows: dose-normalized Cmax/dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC0−t/dose was 1654, 3703, and 1664 ng•h/mL/(mg/kg); T1/2 is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%[2].
Contezolid (MRX-I) exhibits no obvious toxicity[2].
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice infected intranasally with M. tuberculosis Erdman[3].
Dosage: 100, 50 (twice), 25 (twice) mg/kg.
Administration: Gavage, once or twice daily, five days per week for four weeks.
Result: Significantly reduced the CFU recovered from the lungs compared to the early and late control mice (P < 0.05).
Twice daily MRX-I at 50mg/kg and 25 mg/kg were significantly better than the late control mice (P < 0.05).
Once daily MRX-I at 100 mg/kg was significantly better than twice daily 50 mg/kg and 25 mg/kg (P < 0.05). There was no statistical difference between twice daily 50 mg/kg of MRX-I and 25mg/kg (P > 0.05).
Animal Model: Rats[2].
Dosage: 20, 100, and 200/300 mg/kg/day.
Administration: Orally twice daily.
Result: No mortality was observed.
Clinical Trial
Molecular Weight

552.33

Formula

C20H17F3N4NaO8P
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC(C(F)=C1N(C=C2)CCC2=O)=C(N(C(O3)=O)C[C@@H]3CN(C4=NOC=C4)[P](OC(C)=O)(O[Na])=O)C=C1F
Shipping

Shipping with dry ice.
Storage

-80°C, stored under nitrogen
Solvent & Solubility
In Vitro: 

DMSO : 180 mg/mL (325.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8105 mL 9.0526 mL 18.1051 mL
5 mM 0.3621 mL 1.8105 mL 3.6210 mL
View the 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, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8105 mL 9.0526 mL 18.1051 mL 45.2628 mL
5 mM 0.3621 mL 1.8105 mL 3.6210 mL 9.0526 mL
10 mM 0.1811 mL 0.9053 mL 1.8105 mL 4.5263 mL
15 mM 0.1207 mL 0.6035 mL 1.2070 mL 3.0175 mL
20 mM 0.0905 mL 0.4526 mL 0.9053 mL 2.2631 mL
25 mM 0.0724 mL 0.3621 mL 0.7242 mL 1.8105 mL
30 mM 0.0604 mL 0.3018 mL 0.6035 mL 1.5088 mL
40 mM 0.0453 mL 0.2263 mL 0.4526 mL 1.1316 mL
50 mM 0.0362 mL 0.1811 mL 0.3621 mL 0.9053 mL
60 mM 0.0302 mL 0.1509 mL 0.3018 mL 0.7544 mL
80 mM 0.0226 mL 0.1132 mL 0.2263 mL 0.5658 mL
100 mM 0.0181 mL 0.0905 mL 0.1811 mL 0.4526 mL
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Contezolid acefosamil sodium Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Contezolid acefosamil1807365-35-0MRX-4MRX4MRX 4BacterialAntibioticMonoamine OxidaseMAOG+bacteriamonoamineoxidasecSSTIMRSAInhibitorinhibitorinhibit

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