| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
(S)-C12-200 does not act through binding to specific biological targets; rather, its “target” is the intracellular endosomal compartment. As an ionizable cationic lipid, its mechanism is physicochemical: it remains neutral in circulation to reduce non-specific interactions; upon cellular uptake, it becomes protonated and positively charged in the acidic endosome, where it interacts electrostatically with negatively charged endosomal membranes, disrupting membrane integrity and facilitating nucleic acid escape into the cytoplasm.
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|---|---|
| ln Vitro |
As a component of lipid nanoparticles, the in vitro function of (S)-C12-200 primarily manifests in mRNA encapsulation and delivery efficiency. Studies show that (S)-C12-200 exhibits higher mRNA delivery efficiency in vitro compared to the racemic C12-200. This lipid has a pKa value of 7.12, a property that determines its protonation capability under acidic pH and endosomal escape efficiency. LNPs containing (S)-C12-200 encapsulating Cre recombinase mRNA efficiently induced tdTomato expression in hepatocytes, endothelial cells, and Kupffer cells in Ai14 reporter mice.
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| ln Vivo |
In the Ai14 reporter mouse model, (S)-C12-200 demonstrates superior mRNA delivery efficiency to the liver compared to its chiral counterpart. Following intravenous administration of LNPs containing (S)-C12-200 encapsulating Cre mRNA, the percentage of tdTomato+ cells (reporter gene-expressing cells) in the liver was significantly higher than that observed with (R)-C12-200-containing LNPs. This result indicates that (S)-C12-200 offers a significant stereoselective advantage for liver-targeted delivery, supporting the concept that substituting racemic ionizable lipids with stereopure lipids can optimize mRNA delivery efficiency. This study was published in the Journal of Controlled Release in 2023.
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| Enzyme Assay |
(S)-C12-200 is not involved in traditional enzyme or receptor binding assays; its cell-free evaluation focuses on physicochemical characterization. A typical protocol includes: 1) Dissolve (S)-C12-200 in anhydrous ethanol to prepare a stock solution (e.g., 10 mg/mL); 2) Measure LNP particle size (target 80-120 nm), polydispersity index, and Zeta potential by dynamic light scattering; 3) Determine pKa value (reference: 7.12) by pH titration, monitoring lipid protonation across pH range (4.0-8.0); 4) Measure mRNA encapsulation efficiency using fluorescent dye methods (e.g., RiboGreen); 5) Observe LNP morphology by transmission electron microscopy.
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| Cell Assay |
The in vitro cell assay protocol for (S)-C12-200 is as follows: 1) Seed target cells (e.g., HepG2 hepatoma cells, HEK293T cells, or primary hepatocytes) in culture plates and culture to 70-80% confluence at 37°C with 5% CO₂; 2) Prepare LNPs containing (S)-C12-200 via microfluidic or ethanol injection methods, encapsulating reporter mRNA (e.g., luciferase mRNA or GFP mRNA); 3) Add LNPs at various concentrations (mRNA dose typically 0.1-5 μg/well) to cell culture medium and incubate for 24-48 hours; 4) Detect GFP expression by fluorescence microscopy or flow cytometry, or quantify by luciferase activity assay; 5) Assess cell viability by CCK-8 assay to evaluate formulation toxicity.
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| Animal Protocol |
The in vivo animal assay protocol for (S)-C12-200, using the Ai14 reporter mouse model as an example: 1) Use 6-8 week old Ai14 transgenic mice (carrying a CAG-loxP-STOP-loxP-tdTomato reporter gene at the Rosa26 locus); 2) Prepare LNPs containing (S)-C12-200 encapsulating Cre recombinase mRNA via microfluidic technology; 3) Administer via tail vein intravenous injection at an mRNA dose of typically 0.2-1 mg/kg; 4) Euthanize animals 24-72 hours post-administration and collect liver tissue; 5) Prepare liver single-cell suspensions or frozen sections, and measure the percentage of tdTomato-positive cells by flow cytometry or fluorescence microscopy; 6) Compare delivery efficiency between (S)-C12-200, (R)-C12-200, and racemate groups to evaluate the impact of stereoconfiguration on in vivo activity.
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| References |
| Molecular Formula |
C70H145N5O5
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|---|---|
| Molecular Weight |
1136.93
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| Exact Mass |
1136.1246
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| Elemental Analysis |
C, 73.95; H, 12.86; N, 6.16; O, 7.04
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| CAS # |
1226552-44-8
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| Related CAS # |
1226777-45-2 (R-isomer); 1226552-44-8 (S-isomer); 1220890-25-4 (racemate)
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| Appearance |
Typically exists as solids at room temperature
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| Density |
0.948±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
1017.6±65.0 °C(predicted)
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| LogP |
0
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| SMILES |
CCCCCCCCCC[C@@H](CN(CCN1CCN(CC1)CCN(C[C@H](CCCCCCCCCC)O)C[C@H](CCCCCCCCCC)O)CCN(C[C@H](CCCCCCCCCC)O)C[C@H](CCCCCCCCCC)O)O
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| Synonyms |
(S)-C12-200; 1226552-44-8; orb2814117; SCHEMBL19071910; (S)-C12-200 (solution in ethanol);
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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 | 0.8796 mL | 4.3978 mL | 8.7956 mL | |
| 5 mM | 0.1759 mL | 0.8796 mL | 1.7591 mL | |
| 10 mM | 0.0880 mL | 0.4398 mL | 0.8796 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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