Delpazolid

Delpazolid, also known as LCB01-0371, is a new oxazolidinone with cyclic amidrazone. In vitro activity of LCB01-0371 against 624 clinical isolates was evaluated and compared with those of linezolid, vancomycin, and other antibiotics. LCB01-0371 showed good activity against Gram-positive pathogens. In vivo activity of LCB01-0371 against systemic infections in mice was also evaluated. LCB01-0371 was more active than linezolid against these systemic infections. LCB01-0371 showed bacteriostatic activity against Staphylococcus aureus.

Product information

CAS Number: 1219707-39-7

Molecular Weight: 308.31

Formula: C14H17FN4O3

Synonym:

LCB01-0371

LCB-01-0371

Delpazolid

LCB 01-0371

LCB010371

LCB 010371

LCB-010371

Chemical Name: (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

Smiles: CN1CCN(C=N1)C1=CC=C(C=C1F)N1C[C@H](CO)OC1=O

InChiKey: QLUWQAFDTNAYPN-LLVKDONJSA-N

InChi: InChI=1S/C14H17FN4O3/c1-17-4-5-18(9-16-17)13-3-2-10(6-12(13)15)19-7-11(8-20)22-14(19)21/h2-3,6,9,11,20H,4-5,7-8H2,1H3/t11-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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. 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.

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. 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.

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.
2. Kim TS, et al. Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus. Antimicrob Agents Chemother. 2017 Aug 24;61(9).

Products are for research use only. Not for human use.