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Delpazolid (Synonyms: LCB01-0371)

Catalog No.GC19123

Delpazolid is a novel oxazolidinone antibiotic agent which can inhibit the growth of MSSA and MRSA with a MIC90 of 2 ug/mL for both of them.

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Delpazolid Chemical Structure

Cas No.: 1219707-39-7

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25mg
$348.00
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50mg
$616.00
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100mg
$1,105.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

For the in vitro infection procedure, bone marrow-derived macrophages (BMDMs) are plated at a concentration of 2×105 cells/well and infected for 4 h with M. abscessus. The cells are washed with PBS to remove extracellular bacteria and treated with Delpazolid (LCB-0371) in medium for 2 days. Thereafter, the intracellular bacteria are harvested and the lysates are diluted 10 fold in PBS. Each sample is plated on 7H10 agar plates and incubated at 37°C in a 0.5% CO2 incubator for 7 days[2].

Animal experiment:

WT mice are intranasally or intravenously injected with M.Abscessus (1×107 CFU/mouse). After 2 days, the mice are orally administered Delpazolid (LCB-0371) for 4 days, consecutively. At 7 days after M.Abscessus infection, the mice are killed, and their spleens, livers, and lungs are homogenized in PBS. Serial dilutions of the homogenates are plated on 7H10 medium supplemented with 10% OADC (oleic acid, albumin, dextrose, and catalase)[2].

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).

Background

Delpazolid is a novel oxazolidinone antibiotic agent which can inhibit the growth of MSSA and MRSA with a MIC90 of 2 ug/mL for both of them.

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 ug/mL). Delpazolid dramatically decreases the number of intracellular mycobacteria present at 2 days after infection at concentrations of 0.1, 1, and 10 ug/mL[2].

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].

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).

Chemical Properties

Cas No. 1219707-39-7 SDF
Synonyms LCB01-0371
Canonical SMILES O=C1O[C@@H](CO)CN1C2=CC=C(N3C=NN(C)CC3)C(F)=C2
Formula C14H17FN4O3 M.Wt 308.31
Solubility DMSO : 30 mg/mL (97.30 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.2435 mL 16.2174 mL 32.4349 mL
5 mM 0.6487 mL 3.2435 mL 6.487 mL
10 mM 0.3243 mL 1.6217 mL 3.2435 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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