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Contezolid acefosamil sodium

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Catalog No. T36441Cas No. 1807365-35-0

Contezolid acefosamil sodium (MRX-4) is a novel orally active oxazolidinone antibiotic under investigation for the treatment of complicated skin and soft tissue infections (cSSTI) caused by drug-resistant Gram-positive bacteria. It possesses strong efficacy against these pathogens while significantly minimizing the risks of myelosuppression and monoamine oxidase inhibition (MAOI) [1][2].

Contezolid acefosamil sodium

Contezolid acefosamil sodium

😃Good
Catalog No. T36441Cas No. 1807365-35-0
Contezolid acefosamil sodium (MRX-4) is a novel orally active oxazolidinone antibiotic under investigation for the treatment of complicated skin and soft tissue infections (cSSTI) caused by drug-resistant Gram-positive bacteria. It possesses strong efficacy against these pathogens while significantly minimizing the risks of myelosuppression and monoamine oxidase inhibition (MAOI) [1][2].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$764InquiryInquiry
10 mg$1,190InquiryInquiry
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Product Introduction

Bioactivity
Description
Contezolid acefosamil sodium (MRX-4) is a novel orally active oxazolidinone antibiotic under investigation for the treatment of complicated skin and soft tissue infections (cSSTI) caused by drug-resistant Gram-positive bacteria. It possesses strong efficacy against these pathogens while significantly minimizing the risks of myelosuppression and monoamine oxidase inhibition (MAOI) [1][2].
In vitro
Contezolid (MRX-I) demonstrates strong efficacy against a broad spectrum of Gram-positive clinical isolates, including staphylococci, streptococci, and enterococci. Its potency extends to multidrug-resistant (MDR) organisms, such as MRSA, methicillin-resistant Streptococcus epidermidis (MRSE), penicillin-resistant Streptococci (PRSP), and vancomycin-resistant enterococci (VRE)[2].
In vivo
Oral absorption of Contezolid (MRX-I) occurs rapidly in mouse, rat, and dog, with peak plasma concentrations at 0.5-2.6 h postdose. In these species respectively, 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 oral bioavailability is 69%, 109%, and 37%[2]. Contezolid (MRX-I) shows no obvious toxicity [2]. Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to untreated controls[3].
Chemical Properties
Molecular Weight552.33
FormulaC20H17F3N4NaO8P
Cas No.1807365-35-0
SmilesCC(OP([O-])(N(c1nocc1)C[C@H]2CN(c3c(F)c(F)c(N4CCC(C=C4)=O)c(F)c3)C(O2)=O)=O)=O.[Na+]
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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