| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
ZA3-Ep10 targets cellular membranes and undergoes pH-dependent ionization, facilitating endosomal escape of encapsulated RNA payloads. LNPs containing ZA3-Ep10 selectively accumulate in the liver, lung, and kidneys over the heart and spleen in mice. The compound has no direct protein target.
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|---|---|
| ln Vitro |
In vitro, ZA3-Ep10 LNPs demonstrate efficient delivery of mRNA and single-guide RNA (sgRNA) to various cell lines. The LNPs show high transfection efficiency with minimal cytotoxicity, enabling robust gene expression and CRISPR/Cas9-mediated gene editing in cultured cells. Cellular uptake studies confirm LNP internalization via endocytosis.
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| ln Vivo |
In vivo, ZA3-Ep10 LNPs enable successful RNA delivery and non-viral CRISPR/Cas gene editing in mouse models. Following intravenous administration, the LNPs show preferential accumulation in the liver, lung, and kidneys. Studies demonstrate effective gene editing in hepatic tissues with minimal off-target effects. The compound is valuable for therapeutic gene editing applications.
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| Enzyme Assay |
The pKa of ZA3-Ep10 is determined by titration in liposomal formulations. The lipid is incorporated into LNPs with helper lipids and cholesterol, and the apparent pKa is calculated using a pH-sensitive fluorescent dye. Typical values for zwitterionic lipids range from 6-7 for optimal endosomal escape.
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| Cell Assay |
For cell-based assays, adherent cells (e.g., HEK-293, HepG2) are seeded in 96-well plates and treated with ZA3-Ep10 LNPs encapsulating mRNA or sgRNA/Cas9 complexes. After 48-72 hours, transfection efficiency is measured by reporter gene expression (luciferase or GFP). Gene editing efficiency is assessed by T7E1 assays, Sanger sequencing, or flow cytometry for GFP disruption. Cytotoxicity is measured by MTT or CellTiter-Glo assays.
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| Animal Protocol |
For in vivo evaluation, female BALB/c mice are intravenously injected with ZA3-Ep10 LNPs encapsulating Cre recombinase mRNA or CRISPR/Cas9 components. Blood and organs are harvested at various time points for analysis. Gene editing efficiency in tissues is quantified by PCR, sequencing, or by using reporter mice (e.g., Ai14 tdTomato reporter). Biodistribution is assessed by whole-body fluorescence imaging or qRT-PCR for mRNA levels.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for ZA3-Ep10 are limited. When formulated into LNPs, the encapsulated RNA exhibits a circulation half-life of several hours, with predominant accumulation in the liver and lungs. The lipid component is cleared via metabolic pathways. No standalone PK parameters are available.
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| Toxicity/Toxicokinetics |
Toxicity data specific to ZA3-Ep10 are limited. In LNP-formulated studies, no significant acute toxicity or adverse effects have been reported at effective doses. In vitro cytotoxicity assessments in HEK-293 and HepG2 cells show a favorable safety profile.
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| References | |
| Additional Infomation |
ZA3-Ep10 is a research-grade zwitterionic lipid for RNA delivery and gene editing, not approved for human therapy. It is particularly valuable for organ-selective delivery, with preferential accumulation in liver, lung, and kidneys over heart and spleen. No clinical trials are registered for ZA3-Ep10.
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| Molecular Formula |
C66H138N6O9S
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|---|---|
| Molecular Weight |
1191.90173959732
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| Exact Mass |
1191.024
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| CAS # |
2090299-48-0
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| PubChem CID |
132202451
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| Appearance |
White to light yellow ointment
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| LogP |
13.3
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
63
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| Heavy Atom Count |
82
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| Complexity |
1380
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCC(CN(CCC(=O)NCC[N+](C)(C)CCCS(=O)(=O)[O-])CCN(CCN(CC(CCCCCCCC)O)CC(CCCCCCCC)O)CCN(CC(CCCCCCCC)O)CC(CCCCCCCC)O)O
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| InChi Key |
IVEIUBBMCYOZFH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C66H138N6O9S/c1-8-13-18-23-28-33-39-61(73)56-69(46-44-66(78)67-45-54-72(6,7)53-38-55-82(79,80)81)50-47-68(48-51-70(57-62(74)40-34-29-24-19-14-9-2)58-63(75)41-35-30-25-20-15-10-3)49-52-71(59-64(76)42-36-31-26-21-16-11-4)60-65(77)43-37-32-27-22-17-12-5/h61-65,73-77H,8-60H2,1-7H3,(H-,67,78,79,80,81)
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| Chemical Name |
3-[2-[3-[2-[bis[2-[bis(2-hydroxydecyl)amino]ethyl]amino]ethyl-(2-hydroxydecyl)amino]propanoylamino]ethyl-dimethylazaniumyl]propane-1-sulfonate
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~83.90 mM)
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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 | 0.8390 mL | 4.1950 mL | 8.3900 mL | |
| 5 mM | 0.1678 mL | 0.8390 mL | 1.6780 mL | |
| 10 mM | 0.0839 mL | 0.4195 mL | 0.8390 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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