| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Oxazolidinone
It binds to the peptidyl transferase center of the bacterial ribosome, preventing initiation complex formation and protein synthesis. It is bacteriostatic. Its unique structure reduces affinity for mitochondrial ribosomes, accounting for lower mitochondrial toxicity and myelosuppression compared to linezolid. It also has minimal MAO‑A/B inhibition, reducing serotonin syndrome risk. |
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| ln Vitro |
After 24 hours, delapazol (LCB01-0371) demonstrates bacteriostatic activity against MSSA and MRSA at concentrations of 1×MIC and 2×MIC. Delpazolid exhibits bacteriostatic activity at concentrations of 4×MIC and 8×MIC, but after 24 hours of incubation, there is no regrowth at these concentrations[1]. Delpazolid (LCB-0371) (MIC50=1.2 μg/mL) significantly reduces M. abscessus survival. At concentrations of 0.1, 1, and 10 μg/mL, delapazolid significantly reduces the amount of intracellular mycobacteria that are present two days after infection[2].
In vitro, delpazolid shows MIC90 of 0.5‑2 µg/mL against MRSA and S. pneumoniae, and 0.25‑0.5 µg/mL against M. tuberculosis (including MDR strains). It is also active against linezolid‑resistant isolates with G2576T mutation. In time‑kill studies, it shows bactericidal activity at 4x MIC against S. aureus. Cytotoxicity in HepG2 cells: CC50 >200 µM, much higher than linezolid (CC50 ~20 µM). |
| ln Vivo |
Delpazolid (LCB01-0371) exhibits strong protective effects against systemic infections brought on by both Gram-positive and Gram-negative bacteria when taken orally. Delpazolid's ED50 against S. aureus Giorgio (MSSA) infection is 4.53 mg/kg of body weight. Delpazolid's ED50 against S. aureus p125 (MRSA) is 2.96 mg/kg[1]. Seven days after infection, mice's lung colony-forming unit (CFU) counts tend to be lower when Delpazolid (LCB-0371) is given orally at a dose of 100 mg/kg per day (by gavage)[2].
Cellular assays: MIC determination by broth microdilution; time‑kill curves; cytotoxicity by MTT; mitochondrial function by OCR measurement (Seahorse). These confirm lower mitochondrial toxicity. |
| Enzyme Assay |
Non‑cellular assays: ribosomal binding using radiolabeled delpazolid and bacterial ribosomes; cell‑free translation inhibition using E. coli lysate and luciferase reporter.
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| Cell Assay |
In order to perform the in vitro infection process, 2×105 cells/well of bone marrow-derived macrophages (BMDMs) are plated and infected with M. abscessus for 4 hours. After giving the cells a PBS wash to get rid of extracellular bacteria, Delpazolid (LCB-0371) is added to the medium and left for two days. Following the extraction of the intracellular bacteria, the lysates are diluted ten times in PBS. Every sample is plated onto 7H10 agar plates and then incubated for seven days at 37°C in an incubator with 0.5% CO2[2].
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| Animal Protocol |
Intranasal or intravenous injections of M. Abscessus (1×107 CFU/mouse) are given to WT mice. Following a 2-day period, the mice receive Delpazolid (LCB-0371) orally for a consecutive 4-day period. The mice are killed seven days after contracting M. Abscessus, and their livers, lungs, and spleens are homogenized in PBS. The homogenates are plated at serial dilutions on 7H10 medium that has been enhanced with 10% OADC (oleic acid, albumin, dextrose, and catalase)[2].
In vivo, delpazolid has been tested in mouse models of systemic MRSA infection (staphylococcal sepsis). Oral administration (50 mg/kg, b.i.d.) for 3 days reduced bacterial counts in kidney and spleen by 2‑3 log10 CFU, comparable to linezolid. In a murine TB model, delpazolid (100 mg/kg/day) reduced lung CFU by 2.5 log10 after 4 weeks. It was well tolerated with no weight loss. |
| ADME/Pharmacokinetics |
Pharmacokinetics in animals: oral bioavailability ~80% in rats, half‑life ~3‑4 h, good tissue penetration (lung and kidney). In humans, phase 1 trials show Tmax ~1.5 h, half‑life ~4 h, and linear PK. Metabolism via CYP450, renal excretion.
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| Toxicity/Toxicokinetics |
Toxicology: in animal studies, no myelosuppression or neuropathy at therapeutic doses. High doses (200 mg/kg) caused mild GI effects. No genotoxicity or cardiotoxicity (hERG IC50 >100 µM).
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| References | |
| Additional Infomation |
Delpazolid (LCB01-0371) is being studied in the clinical trial NCT01554995 (a randomized, double-blind, placebo-controlled, single-dose clinical study).
Delpazolid is an investigational drug currently in phase 2 clinical trials for tuberculosis and acute skin infections. It is not yet approved. Its improved safety over linezolid makes it a promising candidate for long‑term TB treatment. Further trials are ongoing to confirm efficacy and safety. |
| Molecular Formula |
C14H17FN4O3
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|---|---|
| Molecular Weight |
308.3134
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| Exact Mass |
308.128
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| Elemental Analysis |
C, 54.54; H, 5.56; F, 6.16; N, 18.17; O, 15.57
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| CAS # |
1219707-39-7
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| Related CAS # |
1219707-39-7;
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| PubChem CID |
44205191
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| Appearance |
Solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
481.8±55.0 °C at 760 mmHg
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| Flash Point |
245.2±31.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.645
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| LogP |
-1.05
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
450
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C([H])=C(C([H])=C([H])C=1N1C([H])=NN(C([H])([H])[H])C([H])([H])C1([H])[H])N1C(=O)O[C@@]([H])(C([H])([H])O[H])C1([H])[H]
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| InChi Key |
QLUWQAFDTNAYPN-LLVKDONJSA-N
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| InChi Code |
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
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| 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
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| Synonyms |
Delpazolid; LCB01-0371; LCB 01-0371; LCB-01-0371; LCB010371; LCB 010371; LCB-010371.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~30 mg/mL (~97.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (8.11 mM) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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