PAβN dihydrochloride (MC-207,110 dihydrochloride)
(Synonyms: 苯丙氨酸-精氨酸-Β-萘胺,MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride) 目录号 : GC32063PAβN dihydrochloride (MC-207,110 dihydrochloride)是一种肽模拟化合物,是一种广谱细菌外排泵抑制剂(EPI)。
Cas No.:100929-99-5
Sample solution is provided at 25 µL, 10mM.
PAβN dihydrochloride (MC-207,110 dihydrochloride) is a peptide mimetic compound that is a broad-spectrum bacterial efflux pump inhibitor (EPI)[1]. PAβN dihydrochloride is the first inhibitor of the resistance nodule cell differentiation (RND) family of efflux pumps in Gram-negative bacteria[2]. PAβN dihydrochloride reduces the resistance of Pseudomonas aeruginosa to fluoroquinolones[3]. PAβN dihydrochloride can cause a 2- to 2048-fold decrease in the MIC of antimicrobial agents known to be substrates of the CmeABC pump in all Campylobacter strains[4]. PAβN dihydrochloride can be used to evaluate the efficacy of new EPI candidates[5].
In vitro, treatment of Salmonella typhimurium cells with PAβN dihydrochloride (32μM) inhibited efflux activity, increased the accumulation of ethidium (Et+) and tetraphenylphosphine (TPP+) in cells, and stimulated Et+ fluorescence[6].
References:
[1] Y Mahmood H, Jamshidi S, Mark Sutton J, et al. Current advances in developing inhibitors of bacterial multidrug efflux pumps[J]. Current medicinal chemistry, 2016, 23(10): 1062-1081.
[2] Compagne N, Vieira Da Cruz A, Müller R T, et al. Update on the discovery of efflux pump inhibitors against critical priority Gram-negative bacteria[J]. Antibiotics, 2023, 12(1): 180.
[3] Rahbar M, Hamidi-Farahani R, Asgari A, et al. Expression of RND efflux pumps mediated antibiotic resistance in Pseudomonas aeruginosa clinical strains[J]. Microbial Pathogenesis, 2021, 153: 104789.
[4] Martinez A, Lin J. Effect of an efflux pump inhibitor on the function of the multidrug efflux pump CmeABC and antimicrobial resistance in Campylobacter[J]. Foodbourne Pathogens & Disease, 2006, 3(4): 393-402.
[5] Blankson G A. Structure-activity studies on bacterial efflux inhibitors[M]. Rutgers The State University of New Jersey, School of Graduate Studies, 2016.
[6] Sakalauskaitė S, Mikalayeva V, Daugelavičius R. Ethidium binding to Salmonella enterica ser. Typhimurium Cells and Salmon sperm DNA[J]. Molecules, 2021, 26(11): 3386.
PAβN dihydrochloride (MC-207,110 dihydrochloride)是一种肽模拟化合物,是一种广谱细菌外排泵抑制剂(EPI)[1]。PAβN dihydrochloride是革兰氏阴性菌中耐药结节细胞分化家族(RND)外排泵的第一个抑制剂[2]。PAβN dihydrochloride降低铜绿假单胞菌对氟喹诺酮类药物的耐药性[3]。PAβN dihydrochloride能够导致所有弯曲杆菌菌株中已知为CmeABC泵底物的抗菌剂的MIC降低2至2048倍[4]。PAβN dihydrochloride能够用于评估新EPI候选物的效率[5]。
在体外,PAβN dihydrochloride(32μM)处理鼠伤寒沙门氏菌细胞,可抑制外排活性,增加细胞中乙锭(Et+)和四苯基磷(TPP+)的积累并刺激Et+荧光[6]。
Cas No. | 100929-99-5 | SDF | |
别名 | 苯丙氨酸-精氨酸-Β-萘胺,MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride | ||
Canonical SMILES | O=C([C@H](CCCNC(N)=N)NC([C@H](CC1=CC=CC=C1)N)=O)NC2=CC(C=CC=C3)=C3C=C2.Cl.Cl | ||
分子式 | C25H32Cl2N6O2 | 分子量 | 519.47 |
溶解度 | DMSO : ≥ 100 mg/mL (192.50 mM);Water : 14.29 mg/mL (27.51 mM) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.925 mL | 9.6252 mL | 19.2504 mL |
5 mM | 0.385 mL | 1.925 mL | 3.8501 mL |
10 mM | 0.1925 mL | 0.9625 mL | 1.925 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
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- Purity: >98.00%
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