CAS 165800-04-4|Eperezolid

Introduction：Basic information about CAS 165800-04-4|Eperezolid, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Eperezolid BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

Common Name	Eperezolid
CAS Number	165800-04-4	Molecular Weight	394.39700
Density	1.37g/cm3	Boiling Point	701.2ºC at 760 mmHg
Molecular Formula	C₁₈H₂₃FN₄O₅	Melting Point	/
MSDS	/	Flash Point	377.9ºC

Names

Name	N-[[(5S)-3-[3-fluoro-4-[4-(2-hydroxyacetyl)piperazin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
Synonym	More Synonyms

Eperezolid BiologicalActivity

Description	Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).IC50 value: 1-4 mg/ml (MIC90, staphylococci) [1]Target: AntibioticEperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. The specific binding of eperezolid is dose dependent and is proportional to the ribosome concentrations. Scatchard analysis of the binding data reveals that the dissociation constant (Kd) is about 20 microM. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase [2]. eperezolid was found to bind only to the 50S subunit, with similar affinity as to the 70S ribosome, and to have no affinity for the 30S subunit [3].
Related Catalog	Signaling Pathways >>Anti-infection >>BacterialResearch Areas >>Infection
References	[1]. Rybak MJ, et al. Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus f [2]. Lin AH, et al. The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother. 1997 Oct;41(10):2127-31. [3]. Zhou CC, et al. 1H nuclear magnetic resonance study of oxazolidinone binding to bacterial ribosomes. Antimicrob Agents Chemother. 2002 Mar;46(3):625-9.

Description

Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).IC50 value: 1-4 mg/ml (MIC90, staphylococci) [1]Target: AntibioticEperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. The specific binding of eperezolid is dose dependent and is proportional to the ribosome concentrations. Scatchard analysis of the binding data reveals that the dissociation constant (Kd) is about 20 microM. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase [2]. eperezolid was found to bind only to the 50S subunit, with similar affinity as to the 70S ribosome, and to have no affinity for the 30S subunit [3].

Related Catalog

Signaling Pathways >>Anti-infection >>BacterialResearch Areas >>Infection

References

[1]. Rybak MJ, et al. Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus f

[2]. Lin AH, et al. The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother. 1997 Oct;41(10):2127-31.

[3]. Zhou CC, et al. 1H nuclear magnetic resonance study of oxazolidinone binding to bacterial ribosomes. Antimicrob Agents Chemother. 2002 Mar;46(3):625-9.

Chemical & Physical Properties

Density	1.37g/cm3
Boiling Point	701.2ºC at 760 mmHg
Molecular Formula	C₁₈H₂₃FN₄O₅
Molecular Weight	394.39700
Flash Point	377.9ºC
Exact Mass	394.16500
PSA	102.42000
LogP	0.38670
Vapour Pressure	1.22E-20mmHg at 25°C
Index of Refraction	1.579
InChIKey	SIMWTRCFFSTNMG-AWEZNQCLSA-N
SMILES	CC(=O)NCC1CN(c2ccc(N3CCN(C(=O)CO)CC3)c(F)c2)C(=O)O1
Storage condition	2-8℃

Safety Information

HS Code	2934999090

Customs

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

Eperezolid

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