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Lanopepden

Alias: GSK-322; GSK322; GSK 322; GSK-1322322; GSK1322322; GSK 1322322; GSK-1322322B; GSK-1322322J; GSK 1322322B
Cat No.:V3525 Purity: ≥98%
Lanopepden (formerly known as GSK 1322322 and GSK-322) is a novel, potent and selective peptide deformylase inhibitor with activity againstStaphylococcus aureusstrains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively.
Lanopepden
Lanopepden Chemical Structure CAS No.: 1152107-25-9
Product category: Bacterial
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
2mg
5mg
10mg
25mg
50mg
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Other Forms of Lanopepden:

  • Lanopepden mesylate
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Lanopepden (formerly known as GSK 1322322 and GSK-322) is a novel, potent and selective peptide deformylase inhibitor with activity against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively. It has good in vitro activity against bacteria associated with community-acquired pneumonia and skin infections. Lanopepden had bactericidal activity against S. pneumoniae, H. influenzae, S. pyogenes, and S. aureus, demonstrating a ≥ 3-log(10) decrease in the number of CFU/ml at 4× MIC within 24 h in 29 of the 33 strains tested. Lanopepden represents a valuable alternative therapy for the treatment of infectious diseases caused by drug-resistant pathogens.

Biological Activity I Assay Protocols (From Reference)
References
2015 Sep;59(9):5747-60.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H34N7O4F
Molecular Weight
479.54826
Exact Mass
479.27
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);
Appearance
Solid powder
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 Data
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Concentration-dependent activities of GSK1322322 against extracellular (MHB; pH 7.4 [left panel]) and intracellular (THP-1 monocytes [right panel]) forms of S. aureus strains with different resistance phenotypes (see Table 1 for individual MICs and patterns of resistance to the antistaphylococcal agents tested). Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
  • Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
  • Kinetics of accumulation and release of GSK1322322 in human THP-1 monocytes and murine J774 macrophages. Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
  • Subcellular distribution of [14C]GSK1322322 and of maker enzymes (lactate dehydrogenase, cytosol; cytochrome c-oxidase, mitochondria; N-acetyl-β-hexosaminidase, lysosomes) in homogenates of THP-1 monocytes Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
  • Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
  • Fractionation of cytoplasmic extracts (homogenates minus the N fraction) of J774 macrophages by density equilibration in a linear sucrose gradient (collected in 12 discrete fractions). Antimicrob Agents Chemother.2015 Sep;59(9):5747-60.
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