| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Lanopepden mesylate targets bacterial peptide deformylase (PDF), an essential enzyme for prokaryotic protein maturation. By inhibiting PDF, the compound prevents the correct synthesis of bacterial proteins, leading to antibacterial effects. The compound mainly targets Gram-positive bacteria. Its mechanism of action makes it a valuable tool for studying novel antibiotic mechanisms and developing strategies against drug-resistant bacteria.
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|---|---|
| ln Vitro |
In vitro, Lanopepden mesylate has antibacterial activity by inhibiting the activity of PDF, preventing the correct synthesis of bacterial proteins. Its activity against Gram-positive bacteria, including Staphylococcus aureus, has been characterized. The compound's antibacterial spectrum and potency have been determined in various bacterial strains. Its mechanism of action as a PDF inhibitor has been confirmed.
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| ln Vivo |
In vivo, Lanopepden mesylate has been used in trials studying the treatment of pneumonia, bacterial infections, skin diseases, and skin infections. Its antibacterial efficacy has been evaluated in animal models of infection. The compound's pharmacokinetic properties and tissue distribution have been characterized. Its potential for treating drug-resistant bacterial infections has been investigated.
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| Enzyme Assay |
In cell-free biochemical assays, Lanopepden mesylate is evaluated for its inhibitory activity against peptide deformylase. Enzyme activity assays measure the compound's ability to inhibit PDF-mediated protein maturation. Its purity (>98%) and molecular weight (575.65 g/mol) are characterized using analytical techniques. Its selectivity for bacterial PDF over mammalian enzymes is assessed.
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| Cell Assay |
Cellular assays for Lanopepden mesylate involve evaluating its antibacterial activity against various bacterial strains. Minimum inhibitory concentration (MIC) assays are performed to determine the compound's potency against Gram-positive and Gram-negative bacteria. Its effects on bacterial protein synthesis and viability are studied.
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| Animal Protocol |
Animal models for Lanopepden mesylate include models of bacterial infection, pneumonia, and skin infections. The compound is typically administered via injection or oral routes. Studies have examined its effects on bacterial clearance, survival, and infection resolution. Its pharmacokinetic properties and tissue distribution have been characterized.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Lanopepden mesylate show that the compound has a molecular weight of 575.65 g/mol with a molecular formula of C23H38FN7O7S. The CAS number is 1441390-17-5. The compound is soluble in DMSO. It typically exists as a solid at room temperature. Standard handling procedures for antibacterial agents apply.
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| Toxicity/Toxicokinetics |
The toxicity profile of Lanopepden mesylate has been evaluated in clinical trials. As an antibacterial agent, standard safety precautions for handling pharmaceutical research compounds apply. The compound is for research use only and not for human use except in approved clinical trial settings.
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| Additional Infomation |
Lanopepden mesylate (GSK1322322) is a first-in-class inhibitor of bacterial peptide deformylase with antibacterial activity against Gram-positive bacteria. It has been used in trials for pneumonia and bacterial infections. The CAS number is 1441390-17-5.
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| Molecular Formula |
C23H38FN7O7S
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|---|---|
| Molecular Weight |
575.6574
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| Exact Mass |
575.254
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| CAS # |
1441390-17-5
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| Related CAS # |
1441390-17-5 (mesylate);1152107-25-9;1441390-22-2 (2 mesylate);1441390-28-8 (camsylate);
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| PubChem CID |
71571564
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.069
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
778
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S(C)(=O)(=O)O.FC1=C(N=C(C)N=C1N1CCN2CCOC[C@@H]2C1)NNC([C@@H](CN(C=O)O)CC1CCCC1)=O
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| InChi Key |
UNGNACZMQRGYNV-URBRKQAFSA-N
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| InChi Code |
InChI=1S/C22H34FN7O4.CH4O3S/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;1-5(2,3)4/h14,16-18,33H,2-13H2,1H3,(H,27,32)(H,24,25,26);1H3,(H,2,3,4)/t17-,18+;/m1./s1
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| Chemical Name |
N-[(2R)-3-[2-[6-[(9aS)-3,4,6,7,9,9a-hexahydro-1H-pyrazino[2,1-c][1,4]oxazin-8-yl]-5-fluoro-2-methylpyrimidin-4-yl]hydrazinyl]-2-(cyclopentylmethyl)-3-oxopropyl]-N-hydroxyformamide;methanesulfonic acid
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| Synonyms |
GSK 1322322 mesylate salt GSK-1322322 mesylate salt Lanopepden mesylate GSK1322322 mesylate salt
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7371 mL | 8.6857 mL | 17.3714 mL | |
| 5 mM | 0.3474 mL | 1.7371 mL | 3.4743 mL | |
| 10 mM | 0.1737 mL | 0.8686 mL | 1.7371 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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