| Description | Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is a defensin mimetic antibiotic compound, exhibiting potent anti-infective antimicrobial activity against a range of bacteria. It demonstrates MIC90 values of 1 μg/mL and 8 μg/mL against the Gram-positive bacteria Streptococcus pneumoniae and Streptococcus viridans, respectively. Additionally, it has a MIC90 value of 8 μg/mL for the Gram-negative bacteria Haemophilus influenzae and a MIC90 value of 4 μg/mL for Pseudomonas aeruginosa. |
| In vitro | Both Staphylococcus aureus (SA) and Staphylococcus epidermidis (SE) have the lowest minimum inhibitory concentrations among the bacterial groups. The MIC 90 s to Brilacidin for Streptococcus pneumonia (SP), Streptococcus viridians (SV), Moraxella (MS), Haemophilus influenza (HI), Pseudomonas aeruginosa (PA), and Serratia marcescens (SM) are 4, 32, 256, 32, 16, and 128-fold higher, respectively, than SA and SE. Brilacidin has Gram-positive in vitro activity; topical Brilacidin 0.5% is minimally irritating; and Brilacidin 0.5% was equally efficacious as Vancomycin (VAN) in a methicillin-resistant S. aureus (MRSA) keratitis model when the corneal epithelium is removed. Brilacidin acts primarily on the bacterial cell membrane by depolarization. Brilacidin is more potent for Gram-positive bacteria (except SV) than Gram-negative bacteria[2]. |
| In vivo | Brilacidin demonstrates dose-dependent ocular toxicity after 7 topical instillations (every 30?min for 3?h) in the NZW rabbit ocular toxicity model. Brilacidin 1% is determined to be Mildly Irritating (23.0), Brilacidin 0.5% (6.5), and Brilacidin 0.25% (4.0) are determined to be Minimally Irritating, while Brilacidin 0.1% (2.0) and TBS (1.0) are determined to be Practically Nonirritating and 0.01% Brilacidin (0.5) is determined to be Nonirritating based on their Maximum mean total scores (MMTS) values[2]. |
| Synonyms | PMX 30063 tetrahydrochloride |
| molecular weight | 1082.75 |
| Molecular formula | C40H54Cl4F6N14O6 |
| CAS | 1224095-99-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Bruk Mensa , et al. Comparative Mechanistic Studies of Brilacidin, Daptomycin, and the Antimicrobial Peptide LL16. Antimicrob Agents Chemother. 2014 Sep;58(9):5136-45. 2. Regis P Kowalski, et al. An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-infective. J Ocul Pharmacol Ther. Jan-Feb 2016;32(1):23-7. |
Brilacidin tetrahydrochloride
CAS No.: 1224095-99-1
Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is a defensin mimetic antibiotic compound, exhibiting poten
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