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955094-26-5
  • 馬來(lái)酰亞胺-PEG2-NHS酯

  • names:

    Mal-amido-PEG2-NHS ester

  • CAS號(hào):

    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
馬來(lái)酰亞胺-PEG2-NHS酯
馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來(lái)酰亞胺基團(tuán)和 NHS 酯的,不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于標(biāo)記蛋白質(zhì),胺修飾的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
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中文別名 馬來(lái)酰亞胺-PEG2-NHS酯(955094-26-5);馬來(lái)酰亞胺二聚乙二醇琥珀酰亞胺;馬來(lái)酰亞胺-peg2-磺酰亞胺酯;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;
英文別名 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號(hào) 955094-26-5
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
溶解度Solubility
性狀 Solid
儲(chǔ)藏條件 Storage conditions ?20°攝氏度

馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)實(shí)驗(yàn)注意事項(xiàng):
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡,穿戴防護(hù)服和口罩,佩戴手套,避免與皮膚接觸。
2.實(shí)驗(yàn)過(guò)程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生,必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ),并交于專業(yè)生物廢氣物處理公司處理,以免造成環(huán)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試劑,955094-26-5雜質(zhì),955094-26-5中間體,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購(gòu)買,955094-26-5閃點(diǎn),955094-26-5熔點(diǎn),


產(chǎn)品說(shuō)明 馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來(lái)酰亞胺基團(tuán)和 NHS 酯的,不可切割的ADClinker
Introduction馬來(lái)酰亞胺-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是抗體藥物偶聯(lián)物中的有用保護(hù)基。
Application2馬來(lái)酰亞胺-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
馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)藥理學(xué):
1、馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來(lái)酰亞胺基團(tuán)和 NHS 酯的,不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于標(biāo)記蛋白質(zhì),胺修飾的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
2、馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是具有短氧化萘間隔基的異雙功能交聯(lián)劑,用于將胺基與含多元基化合物或生物分子的連接。馬來(lái)羰基化團(tuán)將與硫化基反應(yīng),而琥珀酸酯基團(tuán)將與胺反應(yīng)。間隔基長(zhǎng)度為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
馬來(lái)酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)參考文獻(xiàn):
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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