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Brilacidin tetrahydrochloride Sale

(Synonyms: PMX 30063 tetrahydrochloride) 目录号 : GC60096

Brilacidintetrahydrochloride(PMX30063tetrahydrochloride)是一种抗菌剂,对革兰氏阳性菌Streptococcuspneumonia和Streptococcusviridans的MIC90分别为1和8μg/mL,对革兰氏阴性菌Haemophilusinfluenza和Pseudomonasaeruginosa的MIC90分别为8和4μg/mL。Brilacidintetrahydrochloride是一种类似防御素的抗生素(antibiotic)。

Brilacidin tetrahydrochloride Chemical Structure

Cas No.:1224095-99-1

规格 价格 库存 购买数量
1mg
¥653.00
现货
5mg
¥1,350.00
现货
10mg
¥2,250.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is an anti-infective antimicrobial with MIC90s of 1 and 8 μg/mL for Gram-positive bacteria Streptococcus pneumonia and Streptococcus viridans, and MIC90 of 8 and 4 μg/mL for Gram-negative bacteria Haemophilus influenza and Pseudomonas aeruginosa. Brilacidin tetrahydrochloride is a defensin mimetic antibiotic compound[1][2].

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[2].

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].

[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.

Chemical Properties

Cas No. 1224095-99-1 SDF
别名 PMX 30063 tetrahydrochloride
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.Cl.Cl.Cl.Cl
分子式 C40H54Cl4F6N14O6 分子量 1082.75
溶解度 DMSO: 83.33 mg/mL (76.96 mM) 储存条件 Store at 2-8°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。
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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.9236 mL 4.6179 mL 9.2357 mL
5 mM 0.1847 mL 0.9236 mL 1.8471 mL
10 mM 0.0924 mL 0.4618 mL 0.9236 mL
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