Size | Price | Stock | Qty |
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100mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
ln Vitro |
DSPC-cholesterol is found in the outer layer of empty lipid nanoparticle (LNP) systems without siRNA, but some of it is internalized with siRNA in loaded systems [2].
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ln Vivo |
RNA interference (RNAi) therapeutics appear to offer substantial opportunities for future therapy. However, post-administration RNAi effectors are typically unable to reach disease target cells in vivo without the assistance of a delivery system or vector. The main focus of this review is on lipid-based nanoparticle (LNP) delivery systems in current research and development that have at least been shown to act as effective delivery systems for functional delivery of RNAi effectors to disease target cells in vivo. The potential utility of these LNP delivery systems is growing rapidly, and LNPs are emerging as the preferred synthetic delivery systems in preclinical studies and current nonviral RNAi effector clinical trials. Moreover, studies on LNP-mediated delivery in vivo are leading to the emergence of useful biophysical parameters and physical organic chemistry rules that provide a framework for understanding in vivo delivery behaviors and outcomes. These same parameters and rules should also suggest ways and means to develop next generations of LNPs with genuine utility and long-term clinical viability[1].
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References |
[1]. Andrew D Miller. Delivery of RNAi therapeutics: work in progress. Expert Rev Med Devices. 2013 Nov;10(6):781-811.
[2]. Jayesh A Kulkarni, et al. On the role of helper lipids in lipid nanoparticle formulations of siRNA. Nanoscale. 2019 Nov 21;11(45):21733-21739. |
Additional Infomation |
Onpattro, the first RNAi-based therapeutic to receive FDA approval, is enabled by a lipid nanoparticle (LNP) system that facilitates siRNA delivery into the cytoplasm of target cells (hepatocytes) following intravenous (i.v.) administration. These LNP-siRNA systems consist of four lipid components (ionizable cationic lipid, distearolyphosphatidycholine or DSPC, cholesterol, and PEG-lipid) and siRNA. The ionizable cationic lipid has been optimised for RNA encapsulation and intracellular delivery, and the PEG-lipids have been engineered to regulate LNP size and transfection potency. The roles of the other "helper" lipids, DSPC and cholesterol, remain less clear. Here we show that in empty LNP systems that do not contain siRNA, DSPC-cholesterol resides in outer layers, whereas in loaded systems a portion of the DSPC-cholesterol is internalised together with siRNA. It is concluded that the presence of internalised helper lipid is vital to the stable encapsulation of siRNA in the LNP and thus to LNP-siRNA function.[2]
1,2-distearoyl-sn-glycero-3-phosphocholine is a phosphatidylcholine 36:0 in which both phosphatidyl acyl groups are specified as stearoyl (octadecanoyl). It is functionally related to an octadecanoic acid. PC(18:0/18:0) is a metabolite found in or produced by Saccharomyces cerevisiae. |
Molecular Formula |
C44H88NO8P
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Molecular Weight |
790.15
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Exact Mass |
789.6247
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Elemental Analysis |
C, 66.88; H, 11.23; N, 1.77; O, 16.20; P, 3.92
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CAS # |
816-94-4
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Related CAS # |
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d70;56952-01-3;1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d74;326495-38-9;1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d79;326495-39-0;1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83;326495-40-3;1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4;326495-35-6;1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d9;326495-36-7;1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d13;326495-37-8
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PubChem CID |
94190
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Appearance |
Typically exists as white to off-white solids at room temperature
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Melting Point |
236 °C
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LogP |
13
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tPSA |
121.0
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SMILES |
P(=O)([O-])(OC([H])([H])[C@@]([H])(C([H])([H])OC(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)OC(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O)OC([H])([H])C([H])([H])[N+](C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
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InChi Key |
NRJAVPSFFCBXDT-HUESYALOSA-N
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InChi Code |
InChI=1S/C44H88NO8P/c1-6-8-10-12-14-16-18-20-22-24-26-28-30-32-34-36-43(46)50-40-42(41-52-54(48,49)51-39-38-45(3,4)5)53-44(47)37-35-33-31-29-27-25-23-21-19-17-15-13-11-9-7-2/h42H,6-41H2,1-5H3/t42-/m1/s1
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Chemical Name |
1,2-Distearoyl-sn-glycero-3-phosphocholine
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Synonyms |
1,2-Distearoyl-sn-glycero-3-PC; 1,2-Distearoyl-sn-glycero-3-phosphocholine; DSPC; Distearoyl phosphatidylcholine; (R)-2,3-Bis(stearoyloxy)propyl (2-(trimethylammonio)ethyl) phosphate; 1,2-dioctadecanoyl-sn-glycero-3-phosphocholine; PC(18:0/18:0); 1,2-Distearoyl-sn-3-phosphacholine;Coatsome MC 8080;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
Ethanol: 12.5 mg/mL (15.82 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (1.58 mM) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (1.58 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (1.58 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.2656 mL | 6.3279 mL | 12.6558 mL | |
5 mM | 0.2531 mL | 1.2656 mL | 2.5312 mL | |
10 mM | 0.1266 mL | 0.6328 mL | 1.2656 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.