Delpazolid (LCB01-0371)

Cas No.:	1219707-39-7
Chemical Name:	Delpazolid
Synonyms:	(R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one;Delpazolid;(5R)-3-[4-(5,6-Dihydro-1-methyl-1,2,4-triazin-4(1H)-yl)-3-fluorophenyl]-5-(hydroxymethyl)-2-oxazolidinone;LCB 01-0371;43EP6XV33E;(5R)-3-[3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one;(5R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)-1,3-oxazolidin-2-one;(5R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one;(5R)-3-[3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4-yl)phenyl]-5-(hydroxymethyl)-1,3-o
SMILES:	FC1C([H])=C(C([H])=C([H])C=1N1C([H])=NN(C([H])([H])[H])C([H])([H])C1([H])[H])N1C(=O)O[C@@]([H])(C([H])([H])O[H])C1([H])[H]
Formula:	C14H17FN4O3
M.Wt:	308.3082
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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].
In Vitro:	Delpazolid (LCB01-0371), at concentrations of 1×MIC and 2×MIC, has bacteriostatic activity against MSSA and MRSA after 24 h. At concentrations of 4×MIC and 8×MIC, Delpazolid shows bacteriostatic activity, but there is no regrowth at concentrations of 4×MIC and 8×MIC after 24 h of incubation[1]. The survival of M. abscessus is greatly decreased in the presence of Delpazolid (LCB-0371) (MIC50=1.2 μg/mL). Delpazolid dramatically decreases the number of intracellular mycobacteria present at 2 days after infection at concentrations of 0.1, 1, and 10 μg/mL[2].