Delpazolid
Delpazolid Basic information
- Product Name:
- Delpazolid
- Synonyms:
-
- Delpazolid
- Delpazolid (LCB01-0371)
- LCB01-0371
- CS-2617
- DELPAZOLID; LCB01-0371; LCB 01-0371; LCB-01-0371; LCB010371; LCB 010371; LCB-010371
- (5R)-3-[4-(5,6-Dihydro-1-methyl-1,2,4-triazin-4(1H)-yl)-3-fluorophenyl]-5-(hydroxymethyl)-2-oxazolidinone
- Delpazolid/(5R)-3-[4-(5,6-Dihydro-1-methyl-1,2,4-triazin-4(1H)-yl)-3-fluorophenyl]-5-(hydroxymethyl)-2-oxazolidinone
- 2-Oxazolidinone, 3-[4-(5,6-dihydro-1-methyl-1,2,4-triazin-4(1H)-yl)-3-fluorophenyl]-5-(hydroxymethyl)-, (5R)-
- CAS:
- 1219707-39-7
- MF:
- C14H17FN4O3
- MW:
- 308.31
- Mol File:
- 1219707-39-7.mol
Delpazolid Chemical Properties
- Boiling point:
- 481.8±55.0 °C(Predicted)
- Density
- 1.44±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:30.0(Max Conc. mg/mL);97.3(Max Conc. mM)
- form
- A crystalline solid
- pka
- 14.05±0.10(Predicted)
- color
- White to off-white
Delpazolid Usage And Synthesis
Description
Delpazolid is an oxazolidinone antibiotic. It is active against a wide range of Gram-positive bacterial clinical isolates, including resistant strains of several species, such as methicillin-resistant S. aureus (MRSA), methicillin-resistant coagulase-negative staphylococci (MRCNS), and penicillin-resistant S. pneumoniae (MICs = 0.125-4 μg/ml). Delpazolid increases survival in mouse models of systemic MRSA, E. faecalis, S. pneumoniae, and H. influenzae infection (ED50s = 2.96, 4.53, 2.28, and 9.96 mg/kg, respectively).
Uses
Delpazolid is a novel oxazolidinone antibiotic agent which can inhibit the growth of MSSA and MRSA with a MIC90 of 2 μg/mL for both of them.
in vivo
When administered orally, Delpazolid (LCB01-0371) shows potent protective effects against systemic infections caused by Gram-positive and Gram-negative bacteria. Against infection caused by S. aureus Giorgio (MSSA), the ED50 of Delpazolid is 4.53 mg/kg of body weight. Against S. aureus p125 (MRSA), the ED50 of Delpazolid is 2.96 mg/kg[1]. When Delpazolid (LCB-0371) is administered at 100 mg/kg daily (by gavage), the colony-forming unit (CFU) counts tend to be decreased in the lungs of mice at 7 days after infection[2].
IC 50
Oxazolidinone
References
[1] Jeong JW, et al. In vitro and in vivo activities of LCB01-0371, a new oxazolidinone. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62. DOI:10.1128/AAC.00723-10
[2] Kim TS, et al. Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus. Antimicrob Agents Chemother. 2017 Aug 24;61(9). DOI:10.1128/AAC.02752-16
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