DMG-PEG 2000
(Synonyms: 1,2-Dimyristoyl-rac-glycero-3-methoxypolyethylene glycol-2000) 目录号 : GC39784
DMG-PEG 2000 is a component for the liposome for siRNA delivery, and improved transfection efficiency in vitro.
Cas No.:160743-62-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human hepatocellular carcinoma cell line Hep3B |
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Preparation Method |
TT2-TT8 were formulated with the helper lipid (1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), 2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) or 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine (POPE)), cholesterol, 1,2-dimyristoyl-sn-glycerol, methoxypolyethylene glycol (DMG-PEG2000) (molar ratio 50/10/38.5/1.5 or based on the orthogonal design table), and FLuc mRNA via pipetting for in vitro studies or via a microfluidic based mixing device for in vivo studies. |
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Reaction Conditions |
Hep3B cells were seeded (2 × 104cells per well) into each well of white 96-well plates in 150 µL of culture medium, allowed to attach overnight in growth medium, and transfected by addition of 20 µL of FLuc mRNA-loaded TT LLNs to growth medium. Transfections were performed in triplicate. After 6 h of transfection, culture medium containing TT LLNs was carefully removed, and 50 µL of serum-free EMEM and 50 µL of Bright-Glo luciferase substrate were mixed and added to each well. |
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Applications |
TT2-TT8 LLNs showed minimal to moderate inhibitory effects on Hep3B cells, and showed a significant positive correlation between transfection efficiency and entrapment efficiency. |
| Animal experiment [1]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
C57BL/6 mice were administered intravenously via tail vein injection with free hFIX mRNA, O-TT3 FLuc (an irrelevant mRNA-loaded LLNs as a control), or O-TT3 hFIX at the indicated dosage. Six hours post administration, blood samples were collected and mixed with an anticoagulant solution (3.2% sodium citrate anticoagulant containing 0.17 mg/mL of corn trypsin inhibitor) in a ratio of 9:1, which was then centrifuged for 15 min at 2500 g. hFIX protein level was measured by enzyme-linked immunosorbent (ELISA) assay. |
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Dosage form |
0.55 mg/kg or 1.1 mg/kg |
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Applications |
Wild-type mice produced 1020 ng/mL hFIX at a dose of 0.55 mg/kg and 2057 ng/mL at a dose of 1.1 mg/kg, respectively. No hFIX was detected in the plasma of mice injected with untreated, free hFIX mRNA-, or TT3 LLNs-treated groups |
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References: [1]: Li B, Luo X, Deng B, et al. An orthogonal array optimization of lipid-like nanoparticles for mRNA delivery in vivo[J]. Nano letters, 2015, 15(12): 8099-8107. |
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DMG-PEG 2000 is a component for the liposome for siRNA delivery, and improved transfection efficiency in vitro [1].
DMG-PEG 2000 is the constituent of the nanoliposomes. The nanoparticles are 60 - 100 nm in size and designed for delivery to hepatocytes. The nanoparticles are formed from a mixture of siRNA and four lipid excipients: 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol, (6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetren-19-yl-4-(dimethylamino) butanoate (DLin-MC3-DMA) and (R)-2,3-bis(tetradecyloxy)propyl 1-(methoxypoly(ethylene glycol)20000)propyl carbamate (DMG-PEG 2000). Both DSPC and cholesterol are well known pharmaceutical ingredients whilst DLin-MC3-DMA and DMG-PEG2000 are novel excipients. Each 1 mL of patisirin contains 3.3 mg DSPC, 6.2 mg cholesterol, 13.0 mg DLin-MC3-DMA and 1.6 mg of DMG-PEG2000 and these lipids associate with the siRNA to form lipid nanoparticles which protects the siRNA from immediate degradation in the circulation and improves delivery to the target site in the liver [2].
References:
[1]. Tianqi Nie, et al. Surface Coating Approach to Overcome Mucosal Entrapment of DNA Nanoparticles for Oral Gene Delivery of Glucagon-like Peptide 1.ACS Appl Mater Interfaces. 2019 Aug 21;11(33):29593-29603.
[2]. Webb C, Forbes N, Roces C B, et al. Using microfluidics for scalable manufacturing of nanomedicines from bench to GMP: A case study using protein-loaded liposomes[J]. International Journal of Pharmaceutics, 2020, 582: 119266.
DMG-PEG 2000 是用于 siRNA 递送的脂质体组分，可提高体外转染效率[1]。
DMG-PEG 2000 是纳米脂质体的成分。纳米粒子的大小为 60-100 nm，专为递送至肝细胞而设计。纳米颗粒由 siRNA 和四种脂质赋形剂的混合物形成:1,2-二硬脂酰-sn-甘油-3-磷酸胆碱 (DSPC)、胆固醇、(6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28 ,31-teren-19-yl-4-(dimethylamino) butanoate (DLin-MC3-DMA) 和 (R)-2,3-bis(tetradecyloxy)propyl 1-(methoxypoly(ethylene glycol)20000)propyl carbamate (DMG -聚乙二醇 2000)。 DSPC 和胆固醇都是众所周知的药物成分，而 DLin-MC3-DMA 和 DMG-PEG2000 是新型赋形剂。每 1 mL patisirin 含有 3.3 mg DSPC、6.2 mg 胆固醇、13.0 mg DLin-MC3-DMA 和 1.6 mg DMG-PEG2000，这些脂质与 siRNA 结合形成脂质纳米颗粒，保护 siRNA 免于在循环中立即降解和改善肝脏中靶点的递送[2]。
| Cas No. | 160743-62-4 | SDF | |
| 别名 | 1,2-Dimyristoyl-rac-glycero-3-methoxypolyethylene glycol-2000 | ||
| Canonical SMILES | CCCCCCCCCCCCCC(OC(COCCOC)COC(CCCCCCCCCCCCC)=O)=O.[n] | ||
| 分子式 | (C2H4O)nC32H62O5 | 分子量 | |
| 溶解度 | DMSO: 100 mg/mL | 储存条件 | Store at 2-8°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。 | ||
| 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 | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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。
Enhanced target cell specificity and uptake of lipid nanoparticles using RNA aptamers and peptides
Beilstein J Org Chem 2021 Apr 26;17:891-907.PMID:33981364DOI:10.3762/bjoc.17.75.
Lipid nanoparticles (LNPs) constitute a facile and scalable approach for delivery of payloads to human cells. LNPs are relatively immunologically inert and can be produced in a cost effective and scalable manner. However, targeting and delivery of LNPs across the blood-brain barrier (BBB) has proven challenging. In an effort to target LNPs composed of an ionizable cationic lipid (DLin-MC3-DMA), cholesterol, the phospholipid 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), and 1,2-dimyristoyl-rac-glycero-3-methoxypolyethylene glycol-2000 (DMG-PEG 2000) to particular cell types, as well as to generate LNPs that can cross the BBB, we developed and assessed two approaches. The first was centered on the BBB-penetrating trans-activator of transcription (Tat) peptide or the peptide T7, and the other on RNA aptamers targeted to glycoprotein gp160 from human immunodeficiency virus (HIV) or C-C chemokine receptor type 5 (CCR5), a HIV-1 coreceptor. We report herein a CCR5-selective RNA aptamer that acts to facilitate entry through a simplified BBB model and that drives the uptake of LNPs into CCR5-expressing cells, while the gp160 aptamer did not. We further observed that the addition of cell-penetrating peptides, Tat and T7, did not increase BBB penetration above the aptamer-loaded LNPs alone. Moreover, we found that these targeted LNPs exhibit low immunogenic and low toxic profiles and that targeted LNPs can traverse the BBB to potentially deliver drugs into the target tissue. This approach highlights the usefulness of aptamer-loaded LNPs to increase target cell specificity and potentially deliverability of central-nervous-system-active RNAi therapeutics across the BBB.