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955094-26-5
  • 马来酰亚胺-PEG2-NHS酯

  • names:

    Mal-amido-PEG2-NHS ester

  • CAS号:

    955094-26-5

    MDL Number: MFCD11041137
  • MF(分子式): C18H23N3O9 MW(分子量): 425.39
  • EINECS: Reaxys Number:
  • Pubchem ID:51340948 Brand:BIOFOUNT
马来酰亚胺-PEG2-NHS酯
马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含马来酰亚胺基团和 NHS 酯的,不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于标记蛋白质,胺修饰的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
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中文别名 马来酰亚胺-PEG2-NHS酯(955094-26-5);马来酰亚胺二聚乙二醇琥珀酰亚胺;马来酰亚胺-peg2-磺酰亚胺酯;2,5-二氧吡咯烷-1-基3-(2-(2-(3-(2,5-二氧代-2H-吡咯-1(5H)-基)丙酰胺基)乙氧基)乙氧基)丙酸酯;
英文别名 Mal-amido-PEG2-NHS ester(955094-26-5);mal-nh-peg2-nhs;Mal-PEG2-NHS;2,5-dioxopyrrolidin-1-yl 3-(2-(2-(3-(2,5-dioxo-2H-pyrrol-1(5H)-yl)propanamido)ethoxy)ethoxy)propanoate;
CAS号 955094-26-5
SMILES O=C(CCOCCOCCNC(CCN1C(C=CC1=O)=O)=O)ON2C(CCC2=O)=O
Inchi InChI=1S/C18H23N3O9/c22-13(5-8-20-14(23)1-2-15(20)24)19-7-10-29-12-11-28-9-6-18(27)30-21-16(25)3-4-17(21)26/h1-2H,3-12H2,(H,19,22)
InchiKey TZPDZOJURBVWHS-UHFFFAOYSA-N
分子式 Formula C18H23N3O9
分子量 Molecular Weight 425.39
闪点 FP
熔点 Melting point 92-94°C
沸点 Boiling point
Polarizability极化度 39.1±0.5 10-24cm3
密度 Density 1.4±0.1 g/cm3
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid
储藏条件 Storage conditions ?20°摄氏度

马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:955094-26-5试剂,955094-26-5杂质,955094-26-5中间体,955094-26-5密度,955094-26-5合成,955094-26-5旋光度,955094-26-5溶解度,955094-26-5购买,955094-26-5闪点,955094-26-5熔点,


产品说明 马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含马来酰亚胺基团和 NHS 酯的,不可切割的ADClinker
Introduction马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5) is a nonclaevableADClinker containing a maleimide group and an NHS ester.
Application1Mal-PEG2-NHS是抗体药物偶联物中的有用保护基。
Application2马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)The NHS ester can be used to label the primary amines (H2) of proteins, amineodified oligonucleotides, and other amineontaining molecules.
Application3
马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)药理学:
1、马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含马来酰亚胺基团和 NHS 酯的,不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于标记蛋白质,胺修饰的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
2、马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是具有短氧化萘间隔基的异双功能交联剂,用于将胺基与含多元基化合物或生物分子的连接。马来羰基化团将与硫化基反应,而琥珀酸酯基团将与胺反应。间隔基长度为17.6埃。
Hansen AM, et al. Microwave-assisted solid-phase synthesis of antisense acpP peptide nucleic acid-peptide conjugates active against colistin- and tigecycline-resistant E. coli and K. pneumoniae. Eur J
Zhang ge, et al. Preparation and application of FAPalpha activated polypeptide magnetic nanosphere compound used for diagnosis of tumors. CN105524141A
马来酰亚胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)参考文献:
1、Microwave-assisted solid-phase synthesis of antisense acpP peptide nucleic acid-peptide conjugates active against colistin- and tigecycline-resistant E. coli and K. pneumoniae
Anna Mette Hansen 1, Gitte Bonke 1, Wouter Frederik Johan Hogendorf 1, Fredrik Björkling 1, John Nielsen 1, Kenneth T Kongstad 1, Dorota Zabicka 2, Magdalena Tomczak 2, Malgorzata Urbas 2, Peter E Nielsen 3, Henrik Franzyk

Abstract Recent discovery of potent antibacterial antisense PNA-peptide conjugates encouraged development of a fast and efficient synthesis protocol that facilitates structure-activity studies. The use of an Fmoc/Boc protection scheme for both PNA monomers and amino acid building blocks in combination with microwave-assisted solid-phase synthesis proved to be a convenient procedure for continuous assembly of antisense PNA-peptide conjugates. A validated antisense PNA oligomer (CTCATACTCT; targeting mRNA of the acpP gene) was linked to N-terminally modified drosocin (i.e., RXR-PRPYSPRPTSHPRPIRV; X = aminohexanoic acid) or to a truncated Pip1 peptide (i.e., RXRRXR-IKILFQNRRMKWKK; X = aminohexanoic acid), and determination of the antibacterial effects of the resulting conjugates allowed assessment of the influence of different linkers as well as differences between the L- and D-forms of the peptides. The drosocin-derived compound without a linker moiety exhibited highest antibacterial activity against both wild-type Escherichia coli and Klebsiella pneumoniae (MICs in the range 2-4 μg/mL ∼ 0.3-0.7 μM), while analogues displaying an ethylene glycol (eg1) moiety or a polar maleimide linker also possessed activity toward wild-type K. pneumoniae (MICs of 4-8 μg/mL ∼ 0.6-1.3 μM). Against two colistin-resistant E. coli strains the linker-deficient compound proved most potent (with MICs in the range 2-4 μg/mL ∼ 0.3-0.7 μM). The truncated all-L Pip1 peptide had moderate inherent activity against E. coli, and this was unaltered or reduced upon conjugation to the antisense PNA oligomer. By contrast, this peptide was 8-fold less potent against K. pneumoniae, but in this case some PNA-peptide conjugates exhibited potent antisense activity (MICs of 2-8 μg/mL ∼ 0.3-1.2 μM). Most interestingly, the antibacterial activity of the D-form peptide itself was 2- to 16-fold higher than that of the L-form, even for the colistin- and tigecycline-resistant E. coli strains (MIC of 1-2 μg/mL ∼ 0.25-0.5 μM). Low activity was found for conjugates with a two-mismatch PNA sequence corroborating an antisense mode of action. Conjugates containing a D-form peptide were also significantly less active. In conclusion, we have designed and synthesized antisense PNA-drosocin conjugates with potent antibacterial activity against colistin- and tigecycline-resistant E. coli and K. pneumonia without concomitant hemolytic properties. In addition, a truncated D-form of Pip1 was identified as a peptide exhibiting potent activity against both wild-type and multidrug-resistant E. coli, P. aeruginosa, and A. baumannii (MICs within the range 1-4 μg/mL ∼ 0.25-1 μM) as well as toward wild-type Staphylococcus aureus (MIC of 2-4 μg/mL ∼ 0.5-1.0 μM). 

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