| Identification | Back Directory | [Name]
Gepotidacin | [CAS]
1075236-89-3 | [Synonyms]
Buagafuran
GSK-2140944
Gepotidacin
Gepotidacin (GSK2140944)
3H,8H-2a,5,8a-Triazaacenaphthylene-3,8-dione, 2-[[4-[[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl]amino]-1-piperidinyl]methyl]-1,2-dihydro-, (2R)- | [Molecular Formula]
C24H28N6O3 | [MDL Number]
MFCD27987926 | [MOL File]
1075236-89-3.mol | [Molecular Weight]
448.52 |
| Chemical Properties | Back Directory | [Boiling point ]
661.9±65.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 7.14 mg/mL (15.92 mM) | [form ]
Solid | [pka]
7.88±0.10(Predicted) | [color ]
White to yellow | [InChIKey]
PZFAZQUREQIODZ-LJQANCHMSA-N | [SMILES]
C1N2C3=C(C=CC2=O)N=CC(=O)N3[C@@H]1CN1CCC(NCC2N=CC3OCCCC=3C=2)CC1 |
| Hazard Information | Back Directory | [Uses]
Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor. | [in vivo]
GSK2140944 MICs are 0.125 to 0.5 mg/L against the six MRSA isolates. ELF penetration ratios range from 1.1 to 1.4. Observed maximal decreases are 1.1 to 3.1 log10 CFU in neutropenic mice. The mean fAUC/MIC ratios required for stasis and 1-log-unit decreases are 59.3 ± 34.6 and 148.4 ± 83.3, respectively. | [storage]
Store at -20°C | [References]
[1] Farrell DJ, et al. In Vitro Activity of Gepotidacin (GSK2140944) against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2017 Feb 23;61(3). DOI:10.1128/AAC.02047-16
[2] Biedenbach DJ, et al. In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens. Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23. DOI:10.1128/AAC.02820-15
[3] O'Riordan W, et al. Efficacy, Safety, and Tolerability of Gepotidacin (GSK2140944) in the Treatment of Patients with Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections. Antimicrob Agents Chemother. 2017 May 24;61(6). DOI:10.1128/AAC.02095-16
[4] So W, et al. Pharmacodynamic Profile of GSK2140944 against Methicillin-Resistant Staphylococcus aureus in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2015 Aug;59(8):4956-61. DOI:10.1128/AAC.00625-15 |
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