| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
OF-02 targets the endosomal membrane, undergoing protonation in the acidic endosomal environment after LNP internalization. This promotes endosomal escape of mRNA and facilitates efficient protein expression in target cells. It has no direct protein target but serves as a delivery vehicle component.
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|---|---|
| ln Vitro |
In vitro, OF-02 formulated into LNPs demonstrates potent transfection of mRNA into various cell lines, including primary cells. It enables high levels of protein expression, such as human erythropoietin (EPO), with favorable cytotoxicity profiles. Comparative studies show OF-02 LNPs outperform benchmark formulations in transfection efficiency across multiple cell types.
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| ln Vivo |
In vivo, OF-02 LNPs deliver mRNA coding for human erythropoietin (EPO) in a mouse model. Following intravenous administration, OF-02 LNPs produce potent and sustained EPO protein expression, leading to dose-dependent increases in hematocrit levels. The compound demonstrates high in vivo potency comparable to or exceeding leading ionizable lipid benchmarks.
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| Enzyme Assay |
For non-cellular evaluation, the pKa of OF-02 is determined by titration in liposomal suspensions using a pH-sensitive fluorescent dye. The compound is dissolved in DMSO and added to buffer solutions across a pH range, and fluorescence changes are monitored to calculate the apparent pKa, typically around 6-7 for optimal endosomal escape.
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| Cell Assay |
For cell-based assays, adherent cells (e.g., HeLa, HEK-293, primary hepatocytes) are seeded in 96-well plates and treated with OF-02 LNPs encapsulating reporter mRNA (luciferase or GFP). After 24-72 hours, transfection efficiency is measured by luminescence, fluorescence microscopy, or flow cytometry. Cytotoxicity is assessed by MTT, CellTiter-Glo, or LDH release assays.
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| Animal Protocol |
For in vivo evaluation, female BALB/c mice are intravenously injected with OF-02 LNPs encapsulating mRNA encoding a reporter protein such as luciferase or erythropoietin. Blood samples are collected at various time points to measure protein expression by ELISA or luminescence assays. Organs (liver, spleen, lung) are harvested for ex vivo imaging or mRNA quantification by qRT-PCR. Formalin-fixed tissues are examined histologically for signs of inflammation or injury.
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| ADME/Pharmacokinetics |
OF-02 is an ionizable lipid with molecular weight 1314.13 g/mol, C84H152N4O6. When formulated into LNPs, it exhibits favorable pharmacokinetics with extended circulation time, predominant accumulation in the liver, and effective endosomal escape. The LNPs show a half-life of several hours to days depending on PEGylation. No standalone PK data are available.
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| Toxicity/Toxicokinetics |
Toxicity data for OF-02 are limited. In LNP-formulated studies, no significant acute toxicity or adverse histological changes have been observed at effective doses in mice. In vitro cytotoxicity assessments in multiple cell lines show a favorable safety profile.
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| References | |
| Additional Infomation |
OF-02 is a research-grade ionizable lipid for mRNA delivery, not approved for human therapy. It is classified as an alkenyl amino alcohol (AAA) lipid and is valuable for developing next-generation LNPs with enhanced potency and reduced immunogenicity. No clinical trials are registered for OF-02.
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| Molecular Formula |
C84H152N4O6
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|---|---|
| Molecular Weight |
1314.13
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| Exact Mass |
1313.171
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| CAS # |
1883431-67-1
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| PubChem CID |
132594335
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| Appearance |
Colorless to light yellow ointment
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| LogP |
25.2
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
70
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| Heavy Atom Count |
94
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| Complexity |
1670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCC/C=C\C/C=C\CCCCCCC(O)CN(CC(O)CCCCCC/C=C\C/C=C\CCCCC)CCCCC1NC(=O)C(NC1=O)CCCCN(CC(O)CCCCCC/C=C\C/C=C\CCCCC)CC(O)CCCCCC/C=C\C/C=C\CCCCC
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| InChi Key |
UMSCHHWDFWCONK-RGLFHLPNSA-N
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| InChi Code |
InChI=1S/C84H152N4O6/c1-5-9-13-17-21-25-29-33-37-41-45-49-53-57-65-77(89)73-87(74-78(90)66-58-54-50-46-42-38-34-30-26-22-18-14-10-6-2)71-63-61-69-81-83(93)86-82(84(94)85-81)70-62-64-72-88(75-79(91)67-59-55-51-47-43-39-35-31-27-23-19-15-11-7-3)76-80(92)68-60-56-52-48-44-40-36-32-28-24-20-16-12-8-4/h21-28,33-40,77-82,89-92H,5-20,29-32,41-76H2,1-4H3,(H,85,94)(H,86,93)/b25-21-,26-22-,27-23-,28-24-,37-33-,38-34-,39-35-,40-36-
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| Chemical Name |
3,6-bis[4-[bis[(9Z,12Z)-2-hydroxyoctadeca-9,12-dienyl]amino]butyl]piperazine-2,5-dione
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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 (e.g. under nitrogen), 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 (~76.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7610 mL | 3.8048 mL | 7.6096 mL | |
| 5 mM | 0.1522 mL | 0.7610 mL | 1.5219 mL | |
| 10 mM | 0.0761 mL | 0.3805 mL | 0.7610 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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