| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
None (excipient). ATX-002 is an ionizable cationic lipid with a pKa of ∼6.0, allowing efficient complexation with RNA at acidic pH and endosomal escape upon endosome acidification. It facilitates delivery of siRNA and mRNA to the cytosol of target cells, especially hepatocytes.
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| ln Vitro |
ATX-002 LNPs efficiently encapsulate siRNA and mRNA (>90% encapsulation). In vitro, ATX-002 LNPs transfect HEK293, HeLa, or HepG2 cells with high efficiency. For siRNA delivery, ATX-002 LNPs achieve >80% target gene knockdown at siRNA concentrations of 1-10 nM. For mRNA delivery, reporter gene expression (e.g., luciferase) is dose-dependent, with maximum expression at 24-48 h post-transfection. ATX-002 LNPs show low cytotoxicity (cell viability >85%).
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| ln Vivo |
In vivo, ATX-002 LNPs have been evaluated for RNA delivery to the liver. Following intravenous administration, ATX-002 LNPs accumulate in the liver and deliver functional siRNA or mRNA to hepatocytes. For example, siRNA against transthyretin (TTR) reduces serum TTR levels by >80% after a single dose. For mRNA delivery, luciferase expression in the liver is detected 6-24 h post-dose. ATX-002 is a property-tunable lipid, allowing optimization of pKa and biodegradability.
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| Enzyme Assay |
ATX-002 (C3₉H₇2N2O₅S, MW 681.06) is a light yellow to yellow ointment soluble in ethanol and DMSO. For LNP preparation, ATX-002 is dissolved in ethanol and mixed with helper lipids (e.g., DSPC, cholesterol, PEG2000-DMG) at optimized molar ratios (e.g., 50:10:38.5:1.5). The mixture is combined with an acidic aqueous buffer (25-50 mM sodium acetate, pH 4-5) containing nucleic acid (siRNA, mRNA) via microfluidic mixing (flow rate ratio 3:1, aqueous:ethanol). LNPs (size 50-150 nm) form spontaneously. Ethanol is removed by dialysis, pH is raised to 7.4, and the pKa of 6.03 is confirmed. Encapsulation efficiency (>90%) is measured by Ribogreen assay. Zeta potential (∼0 to +10 mV at pH 7.4) is measured by DLS.
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| Cell Assay |
For in vitro studies, LNPs are diluted in serum-free medium. HEK293, HeLa, or HepG2 cells are seeded in 96- or 24-well plates (1-2×10⁴ cells/well) and treated with ATX-002 LNPs at RNA doses of 0.1-100 nM (siRNA) or 0.01-1 ug/well (mRNA). After 4-6 h, medium is replaced with complete medium. For siRNA: target gene knockdown is assessed 24-72 h post-transfection by qRT-PCR or Western blot. For mRNA: luciferase activity is measured 24 h post-transfection using a luminescence plate reader; GFP expression is quantified by flow cytometry. Cellular uptake is assessed by fluorescently labeled RNA. Cytotoxicity is evaluated by MTT assay.
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| Animal Protocol |
For in vivo studies, ATX-002 LNPs are administered intravenously via the tail vein to 6-8 week old female BALB/c or C57BL/6 mice at RNA doses of 0.1-1 mg/kg. For siRNA delivery: blood samples are collected at various time points (0, 6, 24, 48, 72 h, 7, 14 d) for serum analysis (e.g., TTR levels by ELISA). For mRNA delivery: bioluminescence imaging is performed 6-24 h post-dose using an IVIS imager after D-luciferin injection. For biodistribution: mice are euthanized 24-72 h post-dose; organs (liver, spleen, kidney, lung) are harvested for ex vivo imaging or RNA quantitation by qRT-PCR. Liver function is assessed by measuring serum ALT/AST.
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| ADME/Pharmacokinetics |
Following i.v. administration, ATX-002 LNPs have a circulation half-life of ∼2-4 h. LNPs accumulate primarily in the liver (∼50-70% of injected dose) and spleen (∼10-20%). The ionizable lipid has a measured pKa of 6.03, enabling efficient endosomal escape. Metabolism likely involves hydrolysis of the ester linkage (the lipid contains a sulfur atom, which may affect metabolic stability). The lipid is cleared via biliary and renal routes. Cmax occurs within 5-30 minutes.
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| Toxicity/Toxicokinetics |
ATX-002 LNPs are generally well-tolerated at siRNA doses ≤1 mg/kg or mRNA doses ≤1 mg/kg. Mild, transient elevation of liver enzymes (ALT, AST) may occur, returning to baseline within 48-72 h. No significant histopathological changes have been reported. Inflammatory cytokine levels (IL-6, TNF-alpha) may be transiently elevated, consistent with LNP administration. ATX-002 is a property-tunable lipid, allowing optimization of biodegradability to reduce potential toxicity. No overt systemic toxicity has been reported.
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| References | |
| Additional Infomation |
ATX-002 (CAS 1777792-34-3, C3₉H₇2N2O₅S, MW 681.06) has >98% purity and is a light yellow to yellow ointment. Storage at -20degC is required. ATX-002 is a research-grade ionizable cationic lipid; no clinical trials or regulatory approvals have been reported. The lipid contains a sulfur atom (thioether) in its tail, which may affect pKa and metabolic stability. ATX-002 is described as a property-tunable lipid for RNA drug delivery; its synthesis and characterization have been described in the literature.
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| Molecular Formula |
C39H72N2O5S
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|---|---|
| Molecular Weight |
681.06
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| Exact Mass |
680.516
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| CAS # |
1777792-34-3
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| PubChem CID |
118084732
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| Appearance |
Light yellow to yellow ointment
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| LogP |
11.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
36
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| Heavy Atom Count |
47
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| Complexity |
750
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCC/C=C\COC(=O)CCCCCCCN(C(=O)SCCN(C)C)CCCCCCCC(=O)OC/C=C\CCCCCC
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| InChi Key |
RGAIHNZNCGOCLA-ZDSKVHJSSA-N
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| InChi Code |
InChI=1S/C39H72N2O5S/c1-5-7-9-11-13-21-27-34-45-37(42)29-23-17-15-19-25-31-41(39(44)47-36-33-40(3)4)32-26-20-16-18-24-30-38(43)46-35-28-22-14-12-10-8-6-2/h21-22,27-28H,5-20,23-26,29-36H2,1-4H3/b27-21-,28-22-
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| Chemical Name |
[(Z)-non-2-enyl] 8-[2-(dimethylamino)ethylsulfanylcarbonyl-[8-[(Z)-non-2-enoxy]-8-oxooctyl]amino]octanoate
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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) |
DMSO: 25 mg/mL (36.71 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 | 1.4683 mL | 7.3415 mL | 14.6830 mL | |
| 5 mM | 0.2937 mL | 1.4683 mL | 2.9366 mL | |
| 10 mM | 0.1468 mL | 0.7341 mL | 1.4683 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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