Murepavadin TFA (POL7080) is a highly potent, specific, macrocycle Pseudomonas antibiotic, activates mast cells via MRGPRX2 and MrgprB2. Murepavadin displays antibacterial activity against a broad panel of multi-drug-resistant P. aeruginosa. Murepavadin induces Ca2+ mobilization, degranulation, chemokine IL-8 and CCL3 production in a human MC line (LAD2 cells) endogenously expressing MRGPRX2. Murepavadin activates human MCs via MRGPRX2 and murine MCs via MrgprB2 and that MRGPRX2 is resistant to β-arrestin-mediated receptor regulation. activates mast cells via MRGPRX2 and MrgprB2. Murepavadin shows potential for the treatment of bacterial infections caused by Pseudomonas aeruginosa.
Physicochemical Properties
M.Wt
1667.83
Formula
C73H112N22O16.C2HF3O2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
cyclo[Ala-Ser-D-Pro-Pro-Thr-Trp-Ile-Dab-Orn-D-Dab-Dab-Trp-Dab-Dab] TFA salt
References
1. Bassetti M, et al. Curr Opin Infect Dis. 2018 Jan 13. doi: 10.1097/QCO.0000000000000438.
