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PAβN dihydrochloride (MC-207,110 dihydrochloride) Sale

(Synonyms: 苯丙氨酸-精氨酸-Β-萘胺,MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride) 目录号 : GC32063

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)。

PAβN dihydrochloride (MC-207,110 dihydrochloride) Chemical Structure

Cas No.:100929-99-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥562.00
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5mg
¥491.00
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10mg
¥687.00
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25mg
¥1,071.00
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50mg
¥1,517.00
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100mg
¥2,410.00
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250mg
¥4,820.00
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Sample solution is provided at 25 µL, 10mM.

Description

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]

化学性质

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
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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
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