購物車 
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馬來酰亞胺-PEG2-NHS酯
- names：
Mal-amido-PEG2-NHS ester
- CAS號：
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
馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來酰亞胺基團和 NHS 酯的，不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于標記蛋白質，胺修飾的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
| 貨品編碼 | 規格 | 純度 | 價格 (￥) | 現價(￥) | 特價(￥) | 庫存描述 | 數量 | 總計 (￥) |
|---|
| 中文別名 | 馬來酰亞胺-PEG2-NHS酯(955094-26-5);馬來酰亞胺二聚乙二醇琥珀酰亞胺;馬來酰亞胺-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 | 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 |
| 儲藏條件 Storage conditions | ?20°攝氏度 |
馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質及有害物質產生，必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
3.實驗后產生的廢棄物需分類存儲，并交于專業生物廢氣物處理公司處理，以免造成環境污染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,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購買,955094-26-5閃點,955094-26-5熔點,
| 產品說明 | 馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來酰亞胺基團和 NHS 酯的，不可切割的ADClinker |
| Introduction | 馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5) is a nonclaevableADClinker containing a maleimide group and an NHS ester. |
| Application1 | Mal-PEG2-NHS是抗體藥物偶聯物中的有用保護基。 |
| Application2 | 馬來酰亞胺-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 |
馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)藥理學：
1、馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來酰亞胺基團和 NHS 酯的，不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于標記蛋白質，胺修飾的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
2、馬來酰亞胺-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劑，用于將胺基與含多元基化合物或生物分子的連接。馬來羰基化團將與硫化基反應，而琥珀酸酯基團將與胺反應。間隔基長度為17.6埃。
1、馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)是包含馬來酰亞胺基團和 NHS 酯的，不可降解 (non-cleavable) 的 ADC linker。NHS ester 可用于標記蛋白質，胺修飾的寡核苷酸和其他含胺分子的伯胺 (-NH2)。
2、馬來酰亞胺-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劑，用于將胺基與含多元基化合物或生物分子的連接。馬來羰基化團將與硫化基反應，而琥珀酸酯基團將與胺反應。間隔基長度為17.6埃。
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續沖洗+P337如果眼睛刺激持續+P2393獲得醫療建議/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
| 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 |
馬來酰亞胺-PEG2-NHS酯(Mal-amido-PEG2-NHS ester,955094-26-5)參考文獻：
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).
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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