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Contezolid

Cat. No. M27802
Contezolid Structure
Synonym:

MRX-I

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Quality Control & Documentation
Biological Activity

Contezolid (MRX-I), 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 (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).

Chemical Information
Molecular Weight 408.33
Formula C18H15F3N4O4
CAS Number 1112968-42-9
Form Solid
Solubility (25°C) DMSO 120 mg/mL (ultrasonic)
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Grace Kaul, et al. Drugs Today (Barc). Contezolid in complicated skin and soft tissue infection

[2] Min Yang, et al. Drug Discov Ther. Prospects of contezolid (MRX-I) against multidrυg-resistant tuberculosis and extensively drυg-resistant tuberculosis

[3] Sheridan M Hoy. Drugs. Correction to: Contezolid: First Approval

[4] Qi Guo, et al. Antimicrob Agents Chemother. A Novel Oxazolidinone, Contezolid (MRX-I), Expresses Anti-Mycobacterium abscessus Activity In Vitro

[5] Sheridan M Hoy. Drugs. Contezolid: First Approval

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Keywords: Contezolid, MRX-I supplier, Antibiotic, inhibitors, activators


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