Brilacidin (PMX 30063)
(Synonyms: PMX 30063) 目录号 : GC32238
Brilacidin (PMX 30063) (PMX 30063) 是一种抗感染抗菌剂，MIC90 为 1 和 8 μ；g/mL 用于革兰氏阳性细菌肺炎链球菌和草绿色链球菌，MIC90 为 8 和 4 μ；g/mL 用于革兰氏-阴性细菌流感嗜血杆菌和铜绿假单胞菌。
Cas No.:1224095-98-0
Sample solution is provided at 25 µL, 10mM.
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Brilacidin is a nonpeptidic anti-infective in a new class of defensin mimetics that is being developed for the treatment of eye infections.
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[1].
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[1].
[1]. Kowalski RP, et al. An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-infective. J Ocul Pharmacol Ther. 2016 Jan-Feb;32(1):23-7.
Cell experiment: | All susceptibility testing is performed by adding 90 μL of bacterial inoculum to 10 μL of 10× serial concentrations of Brilacidin into rows of a 96-well polypropylene plate. Each plate can test 8 bacterial isolates with each row containing a positive growth control and 11 serial dilutions. The diluent of Brilacidin contains 0.01% acetic acid and 0.2% bovine serum albumin. Polypropylene tubes, pipettes, and pipette tips are used to avoid binding of Brilacidin. A 1% stock of Brilacidin is diluted to 1,280 μg/mL and this is serially diluted 2-fold for 10 times to provide testing concentrations. PA and SM are tested starting at 128 μg/mL and ending at 1.25 μg/mL. All other bacteria are tested starting at 64 μg/mL and ending at 0.625 μg/mL. MICs are determined visually by locating the lowest concentration of Brilacidin that inhibits visible bacterial growth (pellet formation). The MICs are tabulated for each bacterial group and reported as MIC50, MIC90, and a range from the lowest to highest MIC[1]. |
Animal experiment: | Rabbits[1] Ocular toxicity was evaluated with 5 concentrations (1%, 0.5%, 0.25%, 0.1%, and 0.01%) of Brilacidin, formulated in Tris-buffered saline (TBS) using the Draize scoring system in the NZW rabbit ocular irritation model. The Draize Scale grades for toxicity to: cornea (opacity-degree of density, area involved), iris, and conjunctiva (redness, chemosis, and discharge). Two rabbits are tested for each Brilacidin concentration and TBS (vehicle control). Rabbits are treated in both eyes with (37 μL) topical drops every 30 min for 3 h (7 total doses). Rabbits are evaluated in a masked fashion for ocular toxicity. Ocular toxicity is evaluated using the Draize scoring system after treatment on day 0 for acute toxicity and on day 4 post treatment for any delayed toxicity. Maximum mean total scores (MMTS) are calculated and eye irritation is classified. |
References: [1]. Kowalski RP, et al. An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-infective. J Ocul Pharmacol Ther. 2016 Jan-Feb;32(1):23-7. | |
| Cas No. | 1224095-98-0 | SDF | |
| 别名 | PMX 30063 | ||
| Canonical SMILES | O=C(C1=NC=NC(C(NC2=CC(C(F)(F)F)=CC(NC(CCCCNC(N)=N)=O)=C2O[C@H]3CNCC3)=O)=C1)NC4=CC(C(F)(F)F)=CC(NC(CCCCNC(N)=N)=O)=C4O[C@H]5CNCC5 | ||
| 分子式 | C40H50F6N14O6 | 分子量 | 936.91 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0673 mL | 5.3367 mL | 10.6734 mL |
| 5 mM | 0.2135 mL | 1.0673 mL | 2.1347 mL |
| 10 mM | 0.1067 mL | 0.5337 mL | 1.0673 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet