| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
DLin-KC2-DMA is novel ionizable and cationic lipid useful for siRNA delivery. DLin-KC2-DMA was formulated and characterized in SNALP and demonstrated to have in vivo activity at siRNA doses as low as 0.01 mg/kg in rodents and 0.1 mg/kg in nonhuman primates.
| ln Vitro |
Significant siRNA-mediated GAPDH gene silencing in macrophages and dendritic cells can be achieved with DLin-KC2-DMA (1, 5 μg; 72 hours) [1]. Dendritic cells and macrophages have a high uptake of DLin-KC2-DMA (24 h) [1]. Following uptake via the endocytic pathway, DLin-KC2-DMA has the ability to efficiently stimulate the release of siRNA that has been encapsulated into the cytosol [1]. In primary APCs, DLin-KC2-DMA is essentially non-toxic [1].
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| ln Vivo |
Target genes in APc can be efficiently silenced in vivo by the DLin-KC2-DMA containing LNP siRNA system (5 mg/kg; intravenous injection; single dose) [1].
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: macrophages, dendritic cells Tested Concentrations: 5 μg/mL (DLin-KC2-DMA contains-LNPs) Incubation Duration: 72 h Experimental Results: Almost no toxicity. Western Blot Analysis[1] Cell Types: macrophages, dendritic cells Tested Concentrations: 1, 5 μg Incubation Duration: 72 hrs (hours) Experimental Results: In macrophages, GAPDH silencing exceeded 60% at 1 μg and over 80 at 5 μg %. Dramatically diminished GAPDH protein, showing 83% silencing effect at 5 μg. |
| Animal Protocol |
Animal/Disease Models: naive C57BL/6 mice[1].
Doses: 3 or 5 mg/kg (DLin-KC2-DMA contains LNP) Route of Administration: Intravenous; single. Experimental Results: GAPDH production was Dramatically diminished in peritoneal macrophages and dendritic cells as well as spleen-derived APCs at the 5 mg/kg dose. |
| References |
| Molecular Formula |
C43H79NO2
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|---|---|
| Molecular Weight |
642.092873811722
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| Exact Mass |
641.611
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| CAS # |
1190197-97-7
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| Related CAS # |
1224373-32-3 (S-isomer);1224373-36-7 (R-isomer);1190197-97-7;
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| PubChem CID |
44464860
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| Appearance |
Colorless to light yellow liquid
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| LogP |
15.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
46
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| Complexity |
704
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCC/C=C\C/C=C\CCCCCCCCC1(OC(CO1)CCN(C)C)CCCCCCCC/C=C\C/C=C\CCCCC
|
| InChi Key |
LRFJOIPOPUJUMI-KWXKLSQISA-N
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| InChi Code |
InChI=1S/C43H79NO2/c1-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-35-38-43(45-41-42(46-43)37-40-44(3)4)39-36-34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-2/h13-16,19-22,42H,5-12,17-18,23-41H2,1-4H3/b15-13-,16-14-,21-19-,22-20-
|
| Chemical Name |
2,2-dilinoleyl-4-dimethylaminoethyl-[1,3]-dioxolane
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| Synonyms |
KC 2 KC-2 KC2
DLin-KC2-DMA D-Lin-KC2-DMA
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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 Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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) |
DMSO : ~100 mg/mL (~155.74 mM)
Ethanol : ~100 mg/mL (~155.74 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO 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: ≥ 2.5 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO 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: ≥ 2.5 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 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 | 1.5574 mL | 7.7871 mL | 15.5741 mL | |
| 5 mM | 0.3115 mL | 1.5574 mL | 3.1148 mL | |
| 10 mM | 0.1557 mL | 0.7787 mL | 1.5574 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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