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Netropsin dihydrochloride Sale

(Synonyms: 纺锤菌素二盐酸; 纺锤菌素) 目录号 : GC36724

A DNA minor groove binder

Netropsin dihydrochloride Chemical Structure

Cas No.:18133-22-7

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1mg
¥1,620.00
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5mg
¥4,500.00
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产品描述

Netropsin is a DNA minor groove binder originally isolated from S. netropsis.1,2 It binds to A/T rich regions of DNA (Ka = 4.9 x 105 M-1 for poly(dA)poly(dT) DNA).3 Netropsin inhibits topoisomerase II (IC90 = 200 ?M in a cell-free assay) and teniposide-induced crosslinks in nuclei from 935.1 mouse fibrosarcoma cells (IC50 = 65 ?M).4 It is active against several bacteria, including S. aureus, S. typhosa, K. pneumoniae, and A. aerogenes with MIC values of 5, 10, 10, and 5 ?g/ml, respectively.2 Netropsin (75 ?g/ml) inhibits viral plaque formation in Shope fibroma virus- or vaccinia virus-infected BS-C-1 host cells.5 It increases survival in a mouse model of endotoxemia induced by LPS when administered at a dose of 25 mg/kg.6

1.Neidle, S.DNA minor-groove recognition by small moleculesNat. Prod. Rep.18(3)291-309(2001) 2.Finlay, A.C., Hochstein, F.A., Sobin, B.A., et al.Netropsin, a new antibiotic produced by a StreptomycesJ. Am. Chem. Soc.73(1)341-343(1951) 3.Wartell, R.M., Larson, J.E., and Wells, R.D.Netropsin. A specific probe for A-T regions of duplex deoxyribonucleic acidJ. Biol. Chem.249(21)6719-6731(1974) 4.Beerman, T.A., Woynarowski, J.M., Sigmund, R.D., et al.Netropsin and bis-netropsin analogs as inhibitors of the catalytic activity of mammalian DNA topoisomerase II and topoisomerase cleavable complexesBiochim. Biophys. Acta1090(1)52-60(1991) 5.Becker, Y., Asher, Y., and Zakay-Rones, Z.Congocidine and distamycin A, antipoxvirus antibioticsAntimicrob. Agents Chemother.1(6)483-488(1972) 6.Grant, M.A., Baron, R.M., Macias, A.A., et al.Netropsin improves survival from endotoxaemia by disrupting HMGA1 binding to the NOS2 promoterBiochem. J.418(1)103-112(2009)

Chemical Properties

Cas No. 18133-22-7 SDF
别名 纺锤菌素二盐酸; 纺锤菌素
Canonical SMILES O=C(C1=CC(NC(CNC(N)=N)=O)=CN1C)NC2=CN(C)C(C(NCCC(N)=N)=O)=C2.[H]Cl.[H]Cl
分子式 C18H28Cl2N10O3 分子量 503.39
溶解度 Soluble in DMSO 储存条件 -20°C, protect from light
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1 mg 5 mg 10 mg
1 mM 1.9865 mL 9.9327 mL 19.8653 mL
5 mM 0.3973 mL 1.9865 mL 3.9731 mL
10 mM 0.1987 mL 0.9933 mL 1.9865 mL
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Research Update

Efficacy of Netropsin dihydrochloride against the viability, cytopathogenicity and hemolytic activity of Trichomonas vaginalis clinical isolates

J Infect Chemother 2019 Dec;25(12):955-964.PMID:31189504DOI:10.1016/j.jiac.2019.05.015.

Trichomonas vaginalis (T. vaginalis) is a common sexually transmitted infection, affecting the urogenital tract. Trichomoniasis is customarily treated with metronidazole (MTZ). MTZ is known to cause undesirable side effects and there is several reports on MTZ resistant T. vaginalis. Thus, the present study aimed to in-vitro evaluate the activity of DNA minor groove binder drug ''Netropsin dihydrochloride'' against metronidazole-sensitive T. vaginalis isolates (G and U isolates) and resistant T. vaginalis isolate (ATCC50138) (R isolate). Netropsin was tested at concentrations ranging from 3.5 to 200 μg/ml. It showed effectiveness against all isolates with MLC of 12.5 μg/ml for G and U isolates and of 25 μg/ml for R isolate. Cytotoxicity assay of isolates exposed to the respective MLC of netropsin for 42 h showed a highly significant reduction in the death percentage of MCDK cell line as compared to the effect elicited by drug free controls. The hemolytic activity was evaluated by hemolytic assay and by monitoring the interaction of T. vaginalis isolates with human erythrocytes by inverted microscopy and scanning electron microscopy. The hemolytic assay showed (0%) hemolysis of RBCs incubated with T. vaginalis isolates treated with the corresponding MLC of netropsin for 24 h. Scanning electron microscopy revealed cytoskeletal deformities of netropsin treated isolates. Taken together, these observations suggest that netropsin is a promising therapy for T. vaginalis infection affecting its viability, virulence, cytopathogenic and hemolytic activity with a mechanism of action that might overcome T. vaginalis resistance to metronidazole.