Netropsin dihydrochloride
(Synonyms: 纺锤菌素二盐酸; 纺锤菌素) 目录号 : GC36724A DNA minor groove binder
Cas No.:18133-22-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >95.00%
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- SDS (Safety Data Sheet)
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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)
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 |
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 | 1.9865 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 |
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 | ||||||||||
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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。
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.