GlpBio

ALC-0315

目录号: GC19792纯度: >98.00%

ALC-0315 是 COVID-19mRNA 疫苗的关键成分，也是核酸治疗研究中备受追捧的脂质。

ALC-0315
Cas No.: 2036272-55-4
规格价格库存数量操作
10mg¥665.00现货
1
25mg¥1,330.00现货
1
50mg¥2,100.00现货
1
100mg¥3,360.00现货
1
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产品描述 Description

ALC-0315 is a key component of the COVID‐19mRNA vaccine and a highly sought-after lipid for nucleic acid therapeutics research [1]. Ionizable cationic lipids are essential for efficient in vivo delivery of RNA by lipid nanoparticles (LNPs). DLin-MC3-DMA (MC3), ALC-0315, and SM-102 are the only ionizable cationic lipids currently clinically approved for RNA therapies. ALC-0315 and SM-102 are structurally similar lipids used in SARS-CoV-2 mRNA vaccines [2].

Cationic lipids (CLs) and ionizable lipids (ILs) initiate the first step of self-assembly via electrostatic interactions. because of toxicity issues and lack of in vivo efficacy, CLs have been replaced by pH-sensitive ILs. The overall architecture of CLs and ILs can be broken down into three parts: (1) the headgroup, (2) the linker, and (3) the tails. The headgroups of ALC-0315 contain a terminal hydroxyl group which could decrease the hydration of the headgroup and improve hydrogen-bonding interactions with the nucleic acid, potentially leading to improved transfection ability. The linker typically connects the headgroup with the tails, although the linkers may also be buried within the tails. DLin-MC3-DMA, ALC-0315, and SM-102 all have ester linkers. DLin-MC3-DMA has two linoleyl tails, while ALC-0315 and SM-102 contain two branched saturated tails that are postulated to endow a cone-shaped geometry, facilitating destabilization of the endosomal membrane and cytosolic release of the nucleic acid [3].

References:
[1]. Saadati F, Cammarone S, Ciufolini M A. A Route to Lipid ALC‐0315: a Key Component of a COVID‐19 mRNA Vaccine[J]. Chemistry–A European Journal, 2022, 28(48): e202200906.
[2]. Ferraresso F, Strilchuk A W, Juang L J, et al. Comparison of DLin-MC3-DMA and ALC-0315 for siRNA Delivery to Hepatocytes and Hepatic Stellate Cells[J]. Molecular Pharmaceutics, 2022.
[3]. Eygeris Y, Gupta M, Kim J, et al. Chemistry of lipid nanoparticles for RNA delivery[J]. Accounts of Chemical Research, 2021, 55(1): 2-12.

ALC-0315 是 COVID-19mRNA 疫苗的关键成分，也是核酸治疗研究中备受追捧的脂质[1]。可电离的阳离子脂质对于通过脂质纳米粒子 (LNP) 在体内有效递送 RNA 至关重要。 DLin-MC3-DMA (MC3)、ALC-0315 和 SM-102 是目前临床上唯一批准用于 RNA 疗法的可电离阳离子脂质。 ALC-0315 和 SM-102 是结构相似的脂质，用于 SARS-CoV-2 mRNA 疫苗[2]。

阳离子脂质 (CL) 和可电离脂质 (IL) 通过静电相互作用启动自组装的第一步。由于毒性问题和缺乏体内功效，CL 已被 pH 敏感的 IL 取代。 CL 和 IL 的整体架构可以分为三个部分:(1) headgroup，(2) linker，和 (3) tails。 ALC-0315 的头部含有一个末端羟基，可以减少头部的水合作用并改善与核酸的氢键相互作用，从而可能提高转染能力。接头通常将头部与尾部连接起来，尽管接头也可以埋在尾部内。 DLin-MC3-DMA、ALC-0315 和 SM-102 都具有酯接头。 DLin-MC3-DMA 有两个亚油基尾巴，而 ALC-0315 和 SM-102 包含两个分支的饱和尾巴，假定它们具有锥形几何形状，促进内体膜的去稳定化和核酸的胞质释放 [3].

实验参考方法 Experimental Reference Method

siRNA–LNP Formulation and Analysis [1]:

Preparation Method

siRNAs were dissolved in sodium acetate (pH 4) and combined with a lipid solution at an amine-to-phosphate (N/P) ratio of 3. The lipid formulations consisted of DSPC, cholesterol, and PEG-DMG at a 10:38.5:1.5% molar ratio, with either 50% DLin-MC3-DMA or ALC-0315. The LNPs were dialyzed against phosphate-buffered saline (PBS) at pH 7.4 in 500-fold excess. For quality control, cholesterol content was measured using the Cholesterol E Assay Kit. To determine siRNA concentration and entrapment, a RiboGreen assay was used. Encapsulation efficiency was measured by comparing Ribogreen signal in LNP samples with or without Triton X-100 detergent. Particle size was measured using a Malvern-Zetasizer Nano.
Animal experiment [2]:

Animal models

C57BL/6J mice

Preparation Method

2′-O-Methylated siRNA targeting murine FVII (siFVII), ADAMTS13 (siADAMTS13) and a negative control siRNA targeting luciferase (siLuc) were used. The resulting LNPs were diluted to a final concentration of 0.1 mg/mL siRNA in PBS prior to intravenous (IV) injection. Injected mice with 1 mg siRNA per kg body weight (mg/kg) for knockdown studies and 5 mg/kg dose for toxicity studies.

Dosage form

1, 5 mg/kg

Applications

Mice treated with siADAMTS13-ALC-0315 at the same dose had greater ADAMTS13mRNA and protein knockdown, compared to mice treated with siADAMTS13-MC3.

References:

[1] : Ferraresso F, Strilchuk A W, Juang L J, et al. Comparison of DLin-MC3-DMA and ALC-0315 for siRNA Delivery to Hepatocytes and Hepatic Stellate Cells[J]. Molecular Pharmaceutics, 2022.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
2036272-55-4
SMILES
OCCCCN(CCCCCCOC(C(CCCCCC)CCCCCCCC)=O)CCCCCCOC(C(CCCCCC)CCCCCCCC)=O
分子式
C₄₈H₉₅NO₅
分子量
766.27 g/mol
溶解性
DMSO : 100 mg/mL (130.50 mM) Ethanol : 100 mg/mL (130.50 mM)
保存条件
4°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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol