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Brilacidin tetrahydrochloride

Catalog No. T38608 CAS 1224095-99-1

Synonyms: PMX 30063 tetrahydrochloride

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.

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Brilacidin tetrahydrochloride Chemical Structure

Brilacidin tetrahydrochloride, CAS 1224095-99-1

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Biological Description

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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) exhibit the lowest minimum inhibitory concentrations (MIC) compared to other bacterial groups studied. The MIC90s for Brilacidin against Streptococcus pneumonia (SP), Streptococcus viridians (SV), Moraxella (MS), Haemophilus influenza (HI), Pseudomonas aeruginosa (PA), and Serratia marcescens (SM) show a marked increase, being 4, 32, 256, 32, 16, and 128 times higher, respectively, than those for SA and SE. Brilacidin demonstrates significant in vitro activity against Gram-positive bacteria, with the exception of SV, and is considerably less effective against Gram-negative bacteria. Topically applied 0.5% Brilacidin solution is minimally irritating and was found to be as effective as Vancomycin (VAN) in a methicillin-resistant S. aureus (MRSA) keratitis model, particularly when the corneal epithelium had been removed. The mechanism of action for Brilacidin primarily involves the depolarization of the bacterial cell membrane, highlighting its potent antibacterial properties, especially against Gram-positive strains.
In vivo	In the NZW rabbit ocular toxicity model, Brilacidin exhibits dose-dependent ocular toxicity following seven topical applications every 30 minutes over a three-hour period. A 1% concentration of Brilacidin is classified as Mildly Irritating with a Maximum mean total score (MMTS) of 23.0. Concentrations of 0.5% (MMTS: 6.5) and 0.25% (MMTS: 4.0) are deemed Minimally Irritating. In contrast, a 0.1% solution of Brilacidin, with an MMTS of 2.0, and TBS with an MMTS of 1.0, are categorized as Practically Nonirritating. Moreover, a 0.01% concentration of Brilacidin, showing an MMTS of 0.5, is identified as Nonirritating.

Synonyms	PMX 30063 tetrahydrochloride
Molecular Weight	1082.75
Formula	C40H54Cl4F6N14O6
CAS No.	1224095-99-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Brilacidin tetrahydrochloride 1224095-99-1 Brilacidin Tetrahydrochloride PMX-30063 PMX 30063 tetrahydrochloride PMX 30063 Tetrahydrochloride Brilacidin PMX30063 Tetrahydrochloride PMX 30063 PMX30063 PMX-30063 Tetrahydrochloride inhibitor inhibit

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