Art. -Nr.: HY-127146

Platensimycin

Name: Platensimycin
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SKU: HY-127146
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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. Nr.: 835876-32-9
Formel: C₂₄H₂₇NO₇
Molecular Weight:441.47

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Platensimycin Chemical Structure

CAS. Nr.: 835876-32-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
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Calculators
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Biologische Aktivität

Beschreibung

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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 P_app 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

Species	Dose	Route	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	T_1/2	T_max	CL_z/F	V_z/F	C_max
Rat^[4]	20 mg/kg	i.p.	30.66 μg/mL·h	35.94 μg/mL·h	0.76 h	0.23 h	0.69 h	0.33 h	0.56 L/h/kg	0.56 L/kg	28.47 μg/mL
Rat^[5]	20 mg/kg	i.p.	59.12 mg·h/L	74.32 mg·h/L	0.79 h	1.32 h	0.89 h	0.2 h	0.27 L/h/kg	0.35 L/kg	54.3 mg/L

In Vivo

Platensimycin (50, 100, 150 μg/h; continuous i.v. infusion; 24 h) reduces renal bacterial burden in mice with disseminated S. aureus infection, with 100 and 150 μg/h decreasing viable counts by 4-5 log and rendering 20% and 40% of kidneys free of detectable viable bacteria, respectively^[1].
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.

Animal Model:

Mice^[1]
Dosage:

50, 100, 150 μg/h
Administration:

i.v.; 24 h
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.

Animal Model:

C57BL/6J (six-week-old)^[3]
Dosage:

10 mg/kg
Administration:

i.p.; at 1 and 5 h post-infection
Result:

Failed to rescue any mice from lethal MRSA peritonitis, with a 0% survival rate.

Animal Model:

C57BL/6J (female, 6-8 weeks old, MRSA-induced acute peritonitis)^[5]
Dosage:

10 mg/kg
Administration:

wice after MRSA challenge
Result:

None of five mice survived beyond 24 h.

Animal Model:

C57BL/6J mice (6-8 weeks old, 18-21 g)^[4]
Dosage:

20 mg/kg
Administration:

i.p.; administered at 1 h and 5 h post-infection
Result:

No mice survived beyond day 2.
Produced survival of all mice.

Chemical Information

CAS. Nr. 835876-32-9
Appearance Solid
Molecular Weight 441.47
Formel C₂₄H₂₇NO₇
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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bioRxiv

2026 Apr 7.

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Data Sheet (296 KB)
SDS (251 KB)
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- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang J, et al. Platensimycin is a selective FabF inhibitor with potent antibiotic properties. Nature. 2006 May 18;441(7091):358-61.

[2]. Cao D, Yang J, Deng Y, Su M, Wang Y, Feng X, Xiong Y, Bai E, Duan Y, Huang Y. Discovery of a mammalian FASN inhibitor against xenografts of non-small cell lung cancer and melanoma. Signal transduction and targeted therapy. 2022 Aug 24;7(1):273.

[3]. Deng Y, et al. Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo. Journal of medicinal chemistry. 2019 Jul 25;62(14):6682-6693.

[4]. Wang Z, Liu X, Peng Y, Su M, Zhu S, Pan J, Shen B, Duan Y, Huang Y. Platensimycin-encapsulated liposomes or micelles as biosafe nanoantibiotics exhibited strong antibacterial activities against methicillin-resistant Staphylococcus aureus infection in mice. Molecular Pharmaceutics. 2020 Jun 10;17(7):2451-62.

[5]. Liu X, et al. Platensimycin-Encapsulated Poly(lactic--glycolic acid) and Poly(amidoamine) Dendrimers Nanoparticles with Enhanced Anti-Staphylococcal Activity . Bioconjugate chemistry. 2020 May 20;31(5):1425-1437.

[6]. Singh SB, Jayasuriya H, Ondeyka JG, Herath KB, Zhang C, Zink DL, Tsou NN, Ball RG, Basilio A, Genilloud O, Diez MT. Isolation, structure, and absolute stereochemistry of platensimycin, a broad spectrum antibiotic discovered using an antisense differential sensitivity strategy. Journal of the American Chemical Society. 2006 Sep 13;128(36):11916-20.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Platensimycin

1 Cited Publications

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Platensimycin

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