| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
None (not a conventional drug target). Ionizable lipid-1 functions as a formulation excipient that interacts with nucleic acids and forms LNPs to enable targeted delivery.
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|---|---|
| ln Vitro |
Ionizable lipid-1 LNPs demonstrate efficient encapsulation of siRNA and mRNA. In HeLa cells, LNP formulations with ionizable lipid-1 achieve high transfection efficiency. The pKa of 6.16 allows for robust endosomal escape, leading to effective gene silencing or protein expression.
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| ln Vivo |
In vivo, ionizable lipid-1 containing LNPs have been used for systemic delivery of siRNA and mRNA in murine models. Typically administered intravenously, these LNPs accumulate in the liver and other tissues, resulting in successful target gene knockdown and reporter protein expression without significant off-target effects.
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| Enzyme Assay |
Ionizable lipid-1 is dissolved in ethanol and mixed with other lipid components (e.g., DSPC, cholesterol, PEG-lipid) at defined molar ratios via microfluidic mixing with an acidic aqueous buffer (e.g., 25 mM sodium acetate, pH 4) containing nucleic acids. LNPs are formed spontaneously, followed by dialysis or tangential flow filtration to remove ethanol and raise pH to 7.4. Particle size (typically 50-150 nm), polydispersity index (PdI), and encapsulation efficiency (>90%) are characterized using dynamic light scattering (DLS) and the Ribogreen assay.
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| Cell Assay |
In vitro cellular uptake and transfection are evaluated using HEK293, HeLa, or primary cells. Cells are seeded in 24- or 96-well plates (2-5×10⁴ cells/well) and incubated with LNP formulations (0.1-10 ug/mL of nucleic acid) for 4-6 h. After 24-48 h, efficacy is measured by flow cytometry for fluorescent reporter proteins (e.g., GFP, luciferase), qPCR for mRNA knockdown, or ELISA for protein expression. Cell viability is assessed via MTT or CellTiter-Glo assays to confirm low cytotoxicity.
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| Animal Protocol |
For in vivo studies, LNPs are administered to 6-8 week old female BALB/c or C57BL/6 mice via intravenous (tail vein) injection at doses of 0.3-1 mg nucleic acid/kg. Biodistribution and efficacy are evaluated 24-72 h post-dose. Organs (liver, spleen, lung, kidney) are harvested for analysis of nucleic acid distribution by qPCR or in vivo imaging (for luciferase or fluorescent reporters), and target gene knockdown is quantified by qRT-PCR or Western blotting.
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| ADME/Pharmacokinetics |
Ionizable lipid-1 demonstrates favorable PK properties typical of LNP-formulated nucleic acids. Following i.v. administration, LNPs have a circulation half-life of 2-6 h, with predominant accumulation in the liver (∼50-70% of injected dose) and spleen (∼10-20%), facilitating efficient delivery to hepatocytes. Lipid clearance occurs via metabolic degradation and biliary excretion.
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| Toxicity/Toxicokinetics |
In preclinical studies, ionizable lipid-1 LNPs are generally well-tolerated at therapeutic doses. Transient and reversible elevations of liver enzymes (ALT/AST) may be observed at high doses. Repeat-dose toxicity studies are needed for advancement. No systemic toxicity has been reported at standard LNP doses of <1 mg/kg.
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| References | |
| Additional Infomation |
Ionizable lipid-1 (CAS 2055939-68-7, C₅₈H114N2O₅, MW 919.5) is research grade with >98% purity. It is typically stored as a powder or in ethanol solution at -20degC under inert atmosphere. This lipid is not approved for human use and is intended for preclinical research applications in nucleic acid delivery (e.g., gene therapy, vaccines). Clinical trials or regulatory approvals have not been reported.
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| Molecular Formula |
C58H114N2O5
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|---|---|
| Molecular Weight |
919.536179065704
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| Exact Mass |
918.872
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| CAS # |
2055939-68-7
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| Related CAS # |
Ionizable lipid-1 hydrochloride
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| PubChem CID |
122666768
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| Appearance |
Colorless to light yellow liquid
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| LogP |
20.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
53
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| Heavy Atom Count |
65
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| Complexity |
954
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(OC(CCCCCC)CCCCCC)(=O)CCCCCCCCC(N(CCCN(C)C)C(=O)CCCCCCC)CCCCCCCCC(OC(CCCCCC)CCCCCC)=O
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| InChi Key |
VBFYPCGDFUFVCZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C58H114N2O5/c1-8-13-18-27-38-48-56(61)60(52-41-51-59(6)7)53(42-32-28-23-25-30-39-49-57(62)64-54(44-34-19-14-9-2)45-35-20-15-10-3)43-33-29-24-26-31-40-50-58(63)65-55(46-36-21-16-11-4)47-37-22-17-12-5/h53-55H,8-52H2,1-7H3
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| Chemical Name |
ditridecan-7-yl 10-[3-(dimethylamino)propyl-octanoylamino]nonadecanedioate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0875 mL | 5.4375 mL | 10.8750 mL | |
| 5 mM | 0.2175 mL | 1.0875 mL | 2.1750 mL | |
| 10 mM | 0.1088 mL | 0.5438 mL | 1.0875 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.
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