1. Anti-infection
  2. Bacterial Antibiotic
  3. Delpazolid

Delpazolid  (Synonyms: LCB01-0371)

Cat. No.: HY-100180 Purity: 98.02%
COA 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 90 In-stock
10 mg USD 140 In-stock
25 mg USD 280 In-stock
50 mg USD 420 In-stock
100 mg USD 590 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Delpazolid

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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

Oxazolidinone

 

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].

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

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].

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

Clinical Trial
Molecular Weight

308.31

Formula

C14H17FN4O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (97.30 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2435 mL 16.2174 mL 32.4349 mL 81.0872 mL
5 mM 0.6487 mL 3.2435 mL 6.4870 mL 16.2174 mL
10 mM 0.3243 mL 1.6217 mL 3.2435 mL 8.1087 mL
15 mM 0.2162 mL 1.0812 mL 2.1623 mL 5.4058 mL
20 mM 0.1622 mL 0.8109 mL 1.6217 mL 4.0544 mL
25 mM 0.1297 mL 0.6487 mL 1.2974 mL 3.2435 mL
30 mM 0.1081 mL 0.5406 mL 1.0812 mL 2.7029 mL
40 mM 0.0811 mL 0.4054 mL 0.8109 mL 2.0272 mL
50 mM 0.0649 mL 0.3243 mL 0.6487 mL 1.6217 mL
60 mM 0.0541 mL 0.2703 mL 0.5406 mL 1.3515 mL
80 mM 0.0405 mL 0.2027 mL 0.4054 mL 1.0136 mL
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Delpazolid Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Delpazolid
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