A bacterial topoisomerase II inhibitor
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Gepotidacin

Item No. 44094

Technical Information
Formal Name
(2R)-2-[[4-[[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl]amino]-1-piperidinyl]methyl]-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione
CAS Number
1075236-89-3
Synonyms
  • GSK2140944
Molecular Formula
C24H28N6O3
Formula Weight
Purity
≥98%
A solid
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1N(C2)C(N3[C@@H]2CN4CCC(CC4)NCC5=NC=C6OCCCC6=C5)=C(N=CC3=O)C=C1
InChi Code
InChI=1S/C24H28N6O3/c31-22-4-3-20-24-29(22)15-19(30(24)23(32)13-27-20)14-28-7-5-17(6-8-28)25-11-18-10-16-2-1-9-33-21(16)12-26-18/h3-4,10,12-13,17,19,25H,1-2,5-9,11,14-15H2/t19-/m1/s1
InChi Key
PZFAZQUREQIODZ-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Gepotidacin is an inhibitor of bacterial topoisomerase II.1 It is active against 84 bacterial clinical isolates (MICs = 0.032-8 µg/ml) and vancomycin-resistant S. aureus (VRSA) and methicillin-resistant S. aureus (MRSA; MICs = 0.125 and 0.25 µg/ml, respectively).1,2 Gepotidacin reduces the number of lung colony-forming units (CFUs) in a mouse model of neutropenic S. aureus lung infection.2 Formulations containing gepotidacin have been used in the treatment of uncomplicated urinary tract infections.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Waites, K.B., Crabb, D.M., Xiao, L., et alIn vitro activities of gepotidacin (GSK2140944) and other antimicrobial agents against human mycoplasmas and ureaplasmas. Antimicrob. Agents Chemother. 61(10), e01064-01017 (2017).

    2. So, W., Crandon, J.L., and Nicolau, D.P. Pharmacodynamic profile of GSK2140944 against methicillin-resistant Staphylococcus aureus in a murine lung infection model. Antimicrob. Agents Chemother. 59(8), 4956-4961 (2015).