Platensimycin
Based on 1 publication(s) in Google Scholar
APOL1-IN-1 is a natural product antibiotic and selective FabF inhibitor discovered in Streptomyces platensis. Platensimycin exhibits IC50 values of 48 nM and 160 nM against Staphylococcus aureus and Escherichia coli FabF, respectively. Platensimycin preferentially recognizes the acyl-enzyme conformation of FabF, occupies the malonyl-binding subsite, and competes with malonyl-ACP, thereby inhibiting bacterial fatty acid elongation. Platensimycin is useful for research on bacterial fatty acid biosynthesis and Gram-positive bacterial infections.
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- CAS No.: 835876-32-9
- Formule: C24H27NO7
- Masse moléculaire:441.47
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Description
In Vitro
Platensimycin inhibits S. aureus and E. coli FabF with IC50 values of 48 nM and 160 nM, respectively, while its IC50 against S. aureus FabH is 67 μM, indicating selective inhibition of FabF[1].
Platensimycin inhibits cellular lipid biosynthesis in S. aureus with an IC50 of 0.1 μg/mL, whereas it does not significantly inhibit DNA, RNA, protein, or cell wall biosynthesis at concentrations up to 500 μg/mL[1].
Platensimycin inhibits cellular lipid biosynthesis in S. pneumoniae with an IC50 of 0.8 μg/mL[1].
Platensimycin inhibits the fatty acid synthase system in the S. aureus FASII cell-free gel elongation assay with an IC50 of 0.2 μg/mL[1].
Platensimycin exhibits antibacterial activity against MSSA, MRSA, VISA, VRE, and S. pneumoniae, with MIC values up to 0.5, 0.5, 0.5, 0.1, and 1 μg/mL, respectively; its MIC against wild-type E. coli is >64 μg/mL, whereas its MIC against efflux-negative E. coli (tolC) is 16 μg/mL[1].
Platensimycin (0.5-64 μg/mL; 16 h) exhibits MICs of 1, 0.5, and 0.5 μg/mL against S. aureus ATCC 29213, clinical MSSA, and MRSA strains, respectively[3].
Platensimycin retains antibacterial activity against 4 clinical MSSA and 45 clinical MRSA isolates, with an MIC of 1.0 μg/mL[3].
Platensimycin (0.125-64 μg/mL; 12 or 24 h) inhibits MRSA growth, and growth inhibition is observed at concentrations below 2 μg/mL[4].
Platensimycin has an MIC of 1 μg/mL against extracellular MRSA, whereas its MIC against intracellular MRSA is >128 μg/mL[4].
Platensimycin (2-8 μg/mL; 24 h) inhibits MRSA biofilm formation[4].
The permeability coefficients of PLGA/PTM and PAMAM/PTM nanoparticles (100 μM) in Caco-2 cell monolayers (4.7 × 10−7 cm s−1 and 6.0 × 10−7 cm s−1, respectively) increase compared with free PTM[5].
Platensimycin (0.5 μg/mL; 24 h) reduces biofilm formation by 88.3% in S. aureus ATCC 29213[5].
Platensimycin binds to the acyl-enzyme state of FabF with a binding IC50 of 19 nM, and the binding signal increases 19-fold relative to apo FabF after formation of the acyl-enzyme intermediate[1].
Platensimycin (100 μg/mL) does not significantly reduce cell viability in RAW 264.7 cells[5].
The apparent permeability coefficient Papp of platensimycin in the Caco-2 monolayer model is 2.4 × 10-7 cm/s[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
Platensimycin (10 mg/kg; i.p.; at 1 and 5 h after bacterial challenge) does not maintain survival in MRSA peritonitis C57BL/6J mice, and none of the PTM group mice survive to the observation endpoint[3].
Platensimycin (50 mg/kg; i.p.; at 1 and 5 h after bacterial challenge) achieves a 50% survival rate in a mouse model of peritonitis infected with 2.5 × 107 CFU MRSA[4].
Platensimycin (20 mg/kg; i.p.; at 1 and 5 h after bacterial challenge) results in survival of all animals in the 1.25 × 107 CFU MRSA peritonitis mouse model, whereas in the more severe model with 2.5 × 107 CFU, no mice survive beyond day 2[4].
Platensimycin (10 mg/kg; i.p.; twice after MRSA challenge) does not maintain survival in C57BL/6J mice with 2.5 × 107 CFU MRSA peritonitis, and none of the 5 mice survive beyond 24 h[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:50, 100, 150 μg/h
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Administration:i.v.; 24 h
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Result:Produced a 4-5 log reduction in viable kidney bacteria at 100 and 150 μg/h.
Yielded no detectable viable bacteria in 20% and 40% of kidneys at 100 and 150 μg/h, respectively.
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Animal Model:C57BL/6J (six-week-old)[3]
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Dosage:10 mg/kg
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Administration:i.p.; at 1 and 5 h post-infection
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Result:Failed to rescue any mice from lethal MRSA peritonitis, with a 0% survival rate.
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Animal Model:C57BL/6J (female, 6-8 weeks old, MRSA-induced acute peritonitis)[5]
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Dosage:10 mg/kg
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Administration:wice after MRSA challenge
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Result:None of five mice survived beyond 24 h.
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Animal Model:C57BL/6J mice (6-8 weeks old, 18-21 g)[4]
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Dosage:20 mg/kg
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Administration:i.p.; administered at 1 h and 5 h post-infection
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Result:No mice survived beyond day 2.
Produced survival of all mice.
Chemical Information
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CAS No. 835876-32-9
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Appearance Solid
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Masse moléculaire 441.47
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Formule C24H27NO7
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(O)C(NC(CC[C@]([C@@]2([H])[C@]34C[C@]5([H])[C@@](C4)(C)O[C@@]2([H])C5)(C)C(C=C3)=O)=O)=C1O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Pureté et documentation
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Fiche technique (296 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
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- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Platensimycin Related Classifications
HY-127146 Related Classifications
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