| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Contezolid acefosamil targets bacterial protein synthesis. As an oxazolidinone antibiotic, it inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. The compound is active against drug-resistant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). It is a prodrug that is converted to the active antibiotic contezolid.
|
|---|---|
| ln Vitro |
Contezolid (MRX-I) is extremely efficient against all clinical isolates of Gram-positive Staphylococcus, Streptococcus, and Enterococcus, including multidrug-resistant (MDR) pathogens including MRSA, PRSP, MRSA, and VRE[2].
In vitro, Contezolid acefosamil is active against drug-resistant Gram-positive bacteria, including MRSA and VRE. As an oxazolidinone antibiotic, it inhibits bacterial protein synthesis. The compound is being evaluated for its activity against a broad spectrum of resistant Gram-positive pathogens. |
| ln Vivo |
Oral absorption of Contezolid (MRX-I) occurs rapidly in mice, rats, and dogs, with peak plasma concentrations seen 0.5−2.6 hours postdose. In mice, rats, and dogs, PK parameters were found as follows: dose-normalized Cmax/dose of 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC0−t/dose of 1654, 3703 and 1664 ng·h/mL/(mg/kg); T1/2 is 1, 1.5, and 3 hours; oral bioavailability is 69%, 109%, and 37% correspondingly [2]. Contezolid (MRX-I) showed no evident toxicity [2]. Contezolid (MRX-I, 100 mg/kg once daily) significantly reduced lung bacterial load compared with untreated early and late controls [3]
In vivo, Contezolid acefosamil is an orally active oxazolidinone antibiotic being studied for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. It is also being evaluated for the treatment of pneumonia. The compound offers a promising alternative to existing antibiotics. |
| Enzyme Assay |
The in vitro antimicrobial susceptibility assay for Contezolid acefosamil involves testing its activity against Gram-positive bacterial pathogens. Bacteria are cultured in the presence of varying compound concentrations, and the minimum inhibitory concentration (MIC) is determined by assessing bacterial growth inhibition. The compound's activity against MRSA and VRE is evaluated.
|
| Cell Assay |
Cellular assays for Contezolid acefosamil are not typically performed, as it is an antibacterial agent. Activity is assessed directly on bacterial cultures rather than on mammalian cells.
|
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse are intranasally infected with Mycobacterium tuberculosis Erdman[3].
Doses: 100, 50 (twice), 25 (twice) mg/kg. Route of Administration: intragastric (po) (po)administration, once or twice (two times) daily, five days a week for four weeks. Experimental Results: CFU recovered from the lungs was Dramatically lower (P < 0.05) compared with early and late control mice. MRX-I at 50 mg/kg and 25 mg/kg twice (two times) daily was Dramatically better than late-stage control mice (P < 0.05). MRX-I at 100 mg/kg one time/day was Dramatically better than 50 mg/kg and 25 mg/kg twice (two times) daily (P < 0.05). There was no statistical difference between 50 mg/kg MRX-I and 25 mg/kg twice (two times) daily (P > 0.05). Animal/Disease Models: Rat[2]. Doses: 20, 100 and 200/300 mg/kg/day. Doses: Take orally twice (two times) daily. Experimental Results: No deaths were observed. In vivo animal studies for Contezolid acefosamil are not detailed in the available sources. The compound is being evaluated in clinical trials for cSSSIs and pneumonia. Specific animal models, dosing regimens, and efficacy data have not been reported in the supplier documentation. |
| ADME/Pharmacokinetics |
Contezolid acefosamil is an orally active compound. It has a molecular weight of 552.3 g/mol and a molecular formula of C20H17F3N4NaO8P. The compound is a prodrug that is converted to the active antibiotic contezolid. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
|
| Toxicity/Toxicokinetics |
Toxicity data for Contezolid acefosamil are not reported in the available sources. As an investigational compound, it has been evaluated in preclinical models and clinical trials. Specific toxicological profiles are not provided in the supplier documentation.
|
| References |
|
| Additional Infomation |
Contezolid acefosamil is an investigational antibiotic being developed for the treatment of complicated skin and soft tissue infections (cSSSIs) and pneumonia caused by resistant Gram-positive bacteria. It is a first-in-class O-acyl phosphoramidate prodrug of the oxazolidinone antibiotic contezolid. The compound is available from chemical suppliers for research purposes.
|
| Molecular Formula |
C20H17F3N4NAO8P
|
|---|---|
| Molecular Weight |
552.329726934433
|
| Exact Mass |
552.063
|
| CAS # |
1807365-35-0
|
| Related CAS # |
Contezolid;1112968-42-9;Contezolid phosphoramidic acid;1807365-43-0;Contezolid acefosamil;1807497-11-5
|
| PubChem CID |
131750213
|
| Appearance |
Off-white to light yellow solid powder
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
37
|
| Complexity |
967
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(=O)OP(=O)(N(C[C@H]1CN(C(=O)O1)C2=CC(=C(C(=C2F)F)N3CCC(=O)C=C3)F)C4=NOC=C4)[O-].[Na+]
|
| InChi Key |
JANNTEAGZXJITO-BTQNPOSSSA-M
|
| InChi Code |
InChI=1S/C20H18F3N4O8P.Na/c1-11(28)35-36(31,32)27(16-4-7-33-24-16)10-13-9-26(20(30)34-13)15-8-14(21)19(18(23)17(15)22)25-5-2-12(29)3-6-25;/h2,4-5,7-8,13H,3,6,9-10H2,1H3,(H,31,32);/q;+1/p-1/t13-;/m1./s1
|
| Chemical Name |
sodium;acetyloxy-[1,2-oxazol-3-yl-[[(5R)-2-oxo-3-[2,3,5-trifluoro-4-(4-oxo-2,3-dihydropyridin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]amino]phosphinate
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~180 mg/mL (~325.89 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.5 mg/mL (8.15 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 45.0 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: ≥ 4.5 mg/mL (8.15 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 45.0 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: ≥ 4.5 mg/mL (8.15 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 | 1.8105 mL | 9.0526 mL | 18.1051 mL | |
| 5 mM | 0.3621 mL | 1.8105 mL | 3.6210 mL | |
| 10 mM | 0.1811 mL | 0.9053 mL | 1.8105 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
