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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 835876-32-9
- 分子式: C24H27NO7
- 分子量:441.47
-
保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-116290
Zaragozic acid A -
HY-N8376
FustinAβ Inhibitor -
HY-113870
6-NBDGFluorescent Dye -
HY-100355S1
C18-Ceramide-d7Stable Isotope -
HY-D0031
8-Aminopyrene-1,3,6-trisulfonic acid trisodiumFluorescent dye -
HY-N12408
GlobotriaosylsphingosineGlobotriaosylceramide -
HY-N0138S
Theobromine-d6Stable Isotope -
HY-100355S
C18-Ceramide-d3Stable Isotope -
HY-17005S
Olmesartan medoxomil-d6Stable Isotope
MedChemExpress（MCE）の使用を引用している文献 Platensimycin
MoreAntibiotic アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
体外実験
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
体内実験
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.
化学情報
-
CAS 番号 835876-32-9
-
性状 Solid
-
分子量 441.47
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
純度とドキュメンテーション
-
データシート (297 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Platensimycin 関連分類
HY-127146 関連分類
Powered by Bioz