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Voxvoganan

Names

[ CAS No. ]:
1166254-80-3

[ Name ]:
Voxvoganan

[Synonym ]:
Lytixar
(2S)-2-amino-5-(diaminomethylideneamino)-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(2-phenylethylamino)pentan-2-yl]amino]-1-oxo-3-(2,5,7-tritert-butyl-1H-indol-3-yl)propan-2-yl]pentanamide
UNII-HO813QDF65

Biological Activity

[Description]:

Voxvoganan (LTX-109), a topical antimicrobial, is highly effective against S. aureus with a MIC range of 2 to 4 μg/mL. Voxvoganan can be used for the research of bacterial skin infections, fungal infections and nasal decolonisation of MRSA[1][2].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Fungal
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Voxvoganan (LTX-109) is an investigational antimicrobial agent with a membrane-lysing mechanism of action, based on the biological principle of innate immune effectors, lytic peptides. Voxvoganan has a rapid bactericidal lytic activity. Voxvoganan demonstrates in vitro bactericidal activity against a number of S. aureus isolates resistant to several classes of antimicrobial agents evaluated in this study[2]. Voxvoganan (LTX-109) is a broad-spectrum, fast-acting bactericidal antimicrobial agent that binds to negatively charged membrane components on the bacterial cell wall, which leads to membrane disruption and cell lysis. Voxvoganan is a first-in-class chemically synthesized, small peptide drug that is stable against protease degradation. Topical application of Voxvoganan has a good safety profile and a low bioavailability. Voxvoganan demonstrates good activity against Staphylococcus aureus strains that are susceptible and resistant to mupirocin[3].

[References]

[1]. Johan Isaksson, et al. A synthetic antimicrobial peptidomimetic (LTX 109): stereochemical impact on membrane disruption. J Med Chem. 2011 Aug 25;54(16):5786-95.

[2]. Louis D Saravolatz, et al. In vitro activities of LTX-109, a synthetic antimicrobial peptide, against methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, daptomycin-nonsusceptible, and linezolid-nonsusceptible Staphylococcus aureus. Antimicrob Agents Chemother. 2012 Aug;56(8):4478-82.

[3]. L D Saravolatz, et al. Postantibiotic effect and postantibiotic sub-MIC effect of LTX-109 and mupirocin on Staphylococcus aureus blood isolates. Lett Appl Microbiol. 2017 Nov;65(5):410-413.

Chemical & Physical Properties

[ Molecular Formula ]:
C43H69N11O3

[ Molecular Weight ]:
788.08000

[ Exact Mass ]:
787.55800

[ PSA ]:
263.38000

[ LogP ]:
9.38830


Related Compounds