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Delpazolid

Cat. No. M6239
Delpazolid Structure
Synonym:

LCB01-0371

Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 320 In stock
50mg USD 1130 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time 2 days
Animal Experiment
Animal models WT mice
Formulation PBS
Dosages 2.96 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 308.31
Formula C14H17FN4O3
CAS Number 1219707-39-7
Purity >98%
Solubility 30 mg/mL in DMSO
Storage at -20°C
References

Activity of LCB01-0371, a Novel Oxazolidinone, against Mycobacterium abscessus.
Kim TS, et al. Antimicrob Agents Chemother. 2017 Aug 24;61(9). PMID: 28674049.

In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
Jeong JW, et al. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62. PMID: 20855730.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Delpazolid, LCB01-0371 supplier, inhibitors

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