DSPE-PEG-Maleimide   中文名称: DSPE-PEG maleimide

DSPE phospholipid for synthesis of lipid carrier

尽管磷脂基纳米载体具有治疗前景，但其广泛临床转化的主要障碍是易受脂肪酸酯水解的影响，导致缺乏质量控制和自组装制剂的不一致。使用电喷雾电离质谱裂解结合基质辅助激光解吸/电离飞行时间质谱，我们证明了一种在纳米载体生产过程中常用的条件下检测聚乙二醇化磷脂DSPE-PEG中一种或两种脂肪酸酯水解的方法。由于此类载体越来越多地用于递送基于肽的治疗药物，我们进一步研究了磷脂酯在固相肽合成和肽高效液相色谱条件下的水解。我们最终详细介绍了一种合成策略，以可靠地生产纯磷脂肽生物偶联物（肽两亲物），同时避免意外或未被注意到的水解副产物，这些副产物可能导致多态性纳米疗法的疗效降低。我们相信，这种方法可以帮助标准化基于磷脂肽的治疗开发、测试和临床翻译。 [1]

[1]. Synthesis and Purification of Homogeneous Lipid-Based Peptide Nanocarriers by Overcoming Phospholipid Ester Hydrolysis. ACS Omega. 2018 Oct 31;3(10):14144-14150.

[2]. Brain drug delivery of small molecules using immunoliposomes. Proc Natl Acad Sci U S A. 1996 Nov 26;93(24):14164-9.

Immunoliposomes (antibody-directed liposomes) were used in the present study for delivery of the antineoplastic agent daunomycin to the rat brain. A coupling procedure was introduced, which allows conjugation of a thiolated antibody to maleimide-grafted 85-nm liposomes sterically stabilized with PEG. Antibody was thereby coupled to the terminal end of a PEG-conjugated linker lipid. No brain uptake of PEG-conjugated liposomes carrying [3H]daunomycin was observed. However, brain targeting of immunoliposomes carrying [3H]daunomycin was mediated by the OX26 monoclonal antibody to the rat transferrin receptor, which is selectively enriched at the brain microvascular endothelium that comprises the blood-brain barrier in vivo. Coupling of 30 OX26 antibodies per liposome resulted in optimal brain delivery. Saturation of delivery was observed at higher antibody densities. Determination of brain levels of immunoliposomes over 24 h revealed that immunoliposomes accumulate in brain tissue. Brain targeting of immunoliposomes was not observed in immunoliposomes conjugated with a mouse IgG2a isotype control. In addition, coinjection of free OX26 saturated plasma clearance of immunoliposomes. Since a single liposome may carry > or = 10,000 drug molecules, the use of PEG-conjugated immunoliposomes increases the drug carrying capacity of the monoclonal antibody by up to 4 logarithmic orders in magnitude. In summary, specific OX26-mediated targeting of daunomycin to the rat brain was achieved by the use of an immunoliposome-based drug delivery system. [1]

(C2H4O)NC51H92N3O13P.H3N

2000

1046.689

474922-22-0

DSPE-PEG2000-Mal ammonium;474922-22-0

163341983

White to off-white solid powder

226

3

14

54

72

1460

0

CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)OCCNC(=O)OCCOCCNC(=O)CCN1C(=O)C=CC1=O)OC(=O)CCCCCCCCCCCCCCCCC.N

HMLYGTOVHVFLDS-UHFFFAOYSA-N

InChI=1S/C53H96N3O14P.H3N/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-51(60)67-45-47(70-52(61)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2)46-69-71(63,64)68-42-39-55-53(62)66-44-43-65-41-38-54-48(57)37-40-56-49(58)35-36-50(56)59;/h35-36,47H,3-34,37-46H2,1-2H3,(H,54,57)(H,55,62)(H,63,64);1H3

azanium;2,3-di(octadecanoyloxy)propyl 2-[2-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxycarbonylamino]ethyl phosphate

474922-22-0; DSPE-PEG2000-MAL; DSPE-PEG(2000) Maleimide; DSPE-PEG(2000)-MAL; azane;[3-[2-[2-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxycarbonylamino]ethoxy-hydroxyphosphoryl]oxy-2-octadecanoyloxypropyl] octadecanoate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Ethanol : ~25 mg/mL
DMF : 10 mg/mL

配方 1 中的溶解度: ≥ 2 mg/mL (Infinity mM) (饱和度未知) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.0 mg/mL 澄清 EtOH 储备液加入到400 μL PEG300中，混匀；再向上述溶液中加入50 μL Tween-80，混匀；然后加入450 μL 生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2 mg/mL (Infinity mM) (饱和度未知) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.0mg/mL澄清EtOH储备液加入到900μL 20％SBE-β-CD生理盐水中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。