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CAS No. : 1224095-99-1
MCE 国际站:Brilacidin tetrahydrochloride
产品活性:Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) 是一种抗菌剂,对革兰氏阳性菌 Streptococcus pneumonia 和 Streptococcus viridans 的 MIC90 分别为 1 和 8 μg/mL,对革兰氏阴性菌 Haemophilus influenza 和 Pseudomonas aeruginosa 的 MIC90 分别为 8 和 4 μg/mL。Brilacidin tetrahydrochloride 是一种类似防御素的抗生素 (antibiotic)。
研究领域:Anti-infection
作用靶点:Bacterial | Antibiotic
In Vitro: Both Staphylococcus aureus (SA) and Staphylococcus epidermidis (SE) have the lowest minimum inhibitory concentrations among the bacterial groups. The MIC90s 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.
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.
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