| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Lanopepden targets bacterial peptide deformylase (PDF), an essential enzyme that removes N‑formyl groups from nascent polypeptides. Inhibition of PDF leads to accumulation of defective proteins, impairing bacterial growth and viability. This target is absent in mammals, providing selectivity.
|
|---|---|
| ln Vitro |
In vitro, lanopepden shows good activity against S. aureus with MICs of 1 mg/L for ATCC 29213 and 25923, and bactericidal activity against S. pneumoniae. Its potency against clinically relevant respiratory and skin pathogens supports its use in bacterial infections.
|
| ln Vivo |
In vivo, lanopepden has been evaluated in preclinical models of pneumonia and skin infections; it shows efficacy in reducing bacterial burden. It has progressed to clinical trials for these indications, though development status may have changed.
|
| Enzyme Assay |
PDF inhibitory activity is measured in cell‑free enzyme assays using recombinant bacterial PDF, a formylated peptide substrate, and varying concentrations of lanopepden; the removal of formyl groups is quantified by HPLC or mass spectrometry to determine IC50.
|
| Cell Assay |
Cell‑based assays involve broth microdilution to determine MIC against bacterial strains, including S. aureus and S. pneumoniae. Bactericidal activity is assessed by time‑kill curves.
|
| Animal Protocol |
In vivo animal models of infection (e.g., mouse thigh or lung infection) are used; lanopepden is administered orally or intravenously, and bacterial colony counts in tissues are measured post‑treatment to evaluate efficacy.
|
| ADME/Pharmacokinetics |
Lanopepden’s PK properties have been studied in preclinical species and early clinical trials; it shows oral bioavailability and appropriate tissue distribution. Detailed half‑life, clearance, and metabolic pathways are not fully public, but it has been used in clinical research.
|
| Toxicity/Toxicokinetics |
Toxicity data are not extensively reported; as a PDF inhibitor, potential concerns include mitochondrial toxicity because mitochondria also contain PDF, but selectivity may mitigate this. Safety studies would be required for clinical development.
|
| References |
Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
|
| Additional Infomation |
Lanopepden has been used in research trials for the treatment of pneumonia, bacterial infections, skin diseases, infectious diseases, and bacterial skin infections.
Lanopepden is an investigational antibacterial not approved; it was developed for community‑acquired pneumonia and skin infections. Its novel mechanism of action offers an alternative to existing antibiotics, but further development status is uncertain; it represents a promising class. |
| Molecular Formula |
C22H34N7O4F
|
|---|---|
| Molecular Weight |
479.54826
|
| Exact Mass |
479.266
|
| Elemental Analysis |
C, 55.10; H, 7.15; F, 3.96; N, 20.45; O, 13.34
|
| CAS # |
1152107-25-9
|
| Related CAS # |
1441390-17-5 (mesylate);1152107-25-9;1441390-22-2 (2 mesylate);1441390-28-8 (camsylate);
|
| PubChem CID |
52918384
|
| Appearance |
Solid powder
|
| LogP |
2.484
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
34
|
| Complexity |
686
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O=CN(C[C@@H](CC1CCCC1)C(NNC2=NC(C)=NC(N3C[C@@]4([H])COCCN4CC3)=C2F)=O)O
|
| InChi Key |
SWHNZGMQMGFQGW-MSOLQXFVSA-N
|
| InChi Code |
InChI=1S/C22H34FN7O4/c1-15-24-20(19(23)21(25-15)29-7-6-28-8-9-34-13-18(28)12-29)26-27-22(32)17(11-30(33)14-31)10-16-4-2-3-5-16/h14,16-18,33H,2-13H2,1H3,(H,27,32)(H,24,25,26)/t17-,18+/m1/s1
|
| Chemical Name |
N-[(2R)-2-(cyclopentylmethyl)-3-(2-{5-fluoro- 6-[(9aS)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]- 2-methylpyrimidin-4-yl}hydrazin-1-yl)-3-oxopropyl]- N-hydroxyformamide
|
| Synonyms |
GSK-322; GSK322; GSK 322; GSK-1322322; GSK1322322; GSK 1322322; GSK-1322322B; GSK-1322322J; GSK 1322322B
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~30 mg/mL (~62.56 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0853 mL | 10.4264 mL | 20.8529 mL | |
| 5 mM | 0.4171 mL | 2.0853 mL | 4.1706 mL | |
| 10 mM | 0.2085 mL | 1.0426 mL | 2.0853 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.
|
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
