Ranbezolid
Ranbezolid (RBx7644 free base) is an orally active, oxazolidinone antibiotic against Gram-positive and Gram-negative anaerobes including Staphylococcus aureus, Staphylococcus epidermidis and Bacteroides fragilis. Ranbezolid can inhibit the 50s ribosomal subunit with an IC50 of 17 μM for bacterial ribosomes. Ranbezolid interferes cell wall and lipid synthesis. Ranbezolid can rapidly kill bacteria, significantly reduce bacterial load, and has better cardiovascular safety. Ranbezolid can be used for the study of antibiotics for anaerobic bacteria.
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- CAS. Nr.: 392659-38-0
- Formel: C21H24FN5O6
- Molecular Weight:461.44
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
Ranbezolid (1 μg/mL) can effectively inhibit protein synthesis in S.aureus as well as in S. epidermidis, and additionally suppress the cell wall and lipid synthesis of Staphylococcus epidermidis[1].
Ranbezoild (1-8 μg/mL) can cause concentration-dependent damage to the cell membrane of S. epidermidis[1].
Ranbezoild exhibits a IC50 value of 17 μM for bacterial ribosomes and safety index of 865[1].
Ranbezolid exhibits the MICs against the anaerobic strains of B. fragilis, B. vulgatus, B. thetaiotaomicron, C. perfringens, C. difficile and P. magnus were 0.06, 0.015, 0.06, 0.06, 0.03 and 0.015 μg/mL, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ranbezoild (≤ 50 mg/kg, p.o., single dose) does not significantly enhance the blood pressure-raising effect of Tyramine (HY-W007606) within the therapeutic dose range in the spontaneous hypertension model of rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine foreign-body infection with Bacteroides fragilis established in swiss albino mice of either sex weighing 20 g[2]
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Dosage:100 mg/kg
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Administration:Oral administration (p.o.), twice daily, for 5 days
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Result:Displayed 5.39log10 reductions.
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Animal Model:Pressor response model established in male Wistar rats (250-350 g)[3]
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Dosage:15, 50 and 100 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Increased mean arterial pressure by 10, 11, 14 mm Hg (15, 50 and 100 mg/kg) with 5 mg/kg Tyramine (HY-W007606).
Chemical Information
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CAS. Nr. 392659-38-0
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Molecular Weight 461.44
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Formel C21H24FN5O6
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SMILES
CC(NC[C@H]1CN(C2=CC=C(N3CCN(CC4=CC=C([N+]([O-])=O)O4)CC3)C(F)=C2)C(O1)=O)=O
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Synonyms
RBx7644 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Kalia V, et al. Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes. Antimicrob Agents Chemother. 2009 Apr;53(4):1427-33. [Content Brief]
[2]. Mathur T, et al. Anti-anaerobic potential of ranbezolid: insight into its mechanism of action against Bacteroides fragilis. Int J Antimicrob Agents. 2013 Jan;41(1):36-40. [Content Brief]
[3]. Naruganahalli KS, et al. Ranbezolid, a novel oxazolidinone antibacterial: in vivo characterisation of monoamine oxidase inhibitory potential in conscious rats. Eur J Pharmacol. 2006 Sep 18;545(2-3):167-72. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Ranbezolid Related Classifications
HY-19428 Related Classifications
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