1. Anti-infection
  2. Bacterial
  3. Delpazolid

Delpazolid (Synonyms: LCB01-0371)

Cat. No.: HY-100180 Purity: 98.22%
Handling Instructions

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.

For research use only. We do not sell to patients.

Delpazolid Chemical Structure

Delpazolid Chemical Structure

CAS No. : 1219707-39-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 211 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
25 mg USD 624 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1104 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1980 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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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.

IC50 & Target

MIC90: 2 μg/mL (MSSA), 2 μg/mL (MRSA)[1]

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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (97.30 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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 6.4870 mL
10 mM 0.3243 mL 1.6217 mL 3.2435 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

308.31

Formula

C₁₄H₁₇FN₄O₃

CAS No.

1219707-39-7

SMILES

O=C1O[[email protected]@H](CO)CN1C2=CC=C(N3C=NN(C)CC3)C(F)=C2

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Delpazolid
Cat. No.:
HY-100180
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Delpazolid

Cat. No.: HY-100180