Formulation: A solid
Formal Name: (S)-N-((2S,5S,8S,11S,14S,17S)-2-((1H-indol-3-yl)methyl)-1,21-diamino-5,8-bis(4-aminobutyl)-11,14-diisopropyl-1,4,7,10,13,16-hexaoxo-3,6,9,12,15-pentaazahenicosan-17-yl)-2-((6S,9S,12S,15S,18S)-9-((1H-indol-3-yl)methyl)-1,6-diamino-12-(4-aminobutyl)-18-benzyl-15-((S)-sec-butyl)-1-imino-7,10,13,16-tetraoxo-2,8,11,14,17-pentaazanonadecan-19-amido)-6-aminohexanamide, trifluoroacetate salt
Purity: ≥95%
Formula Markup: C83H133N23O12 • XCF3COOH
Formula Weight: 1645,1
Shelf life (days): 1460
Notes: Pap12-6 is an antibacterial peptide derived from the twelve N-terminal amino acids of the peptide papiliocin, which has been found in P. xuthus larvae.{51476} It is active against a panel of eight Gram-negative bacteria, including E. coli, P. aeruginosa, and S. syphimurium (MIC50s = 4-8 µM), and the Gram-positive bacteria S. aureus, methicillin-resistant S. aureus 3126 (MRSA-3126), B. subtilis, and S. epidermidis (MIC50s = 4-8 µM) without affecting the viability of human erythrocytes, mouse RAW 264.7 macrophages, human HaCaT keratinocytes, or human HEK293 kidney cells at 25 µM. Pap12-6 induces membrane depolarization in E. coli when used at concentrations of 4 and 8 µM. Preincubation with Pap12-6 (10 µM) reduces nitrite (NO2-), Tnf-α, and Il-6 secretion levels in LPS-stimulated RAW 264.7 macrophages. In vivo, Pap12-6 (10 mg/kg) increases survival in mice infected with E. coli, as well as reduces the number of colony forming units (CFUs) in the lungs, liver, and kidneys in E. coli-infected mice when administered at a dose of 1 mg/kg. Pap12-6 (1 mg/kg) reduces serum aspartate aminotransferase (AST) and alanine transaminase (ALT) levels and blood urea nitrogen levels in a mouse model of E. coli-induced sepsis.
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