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| Targets |
306-O12B-3 does not have a specific biological target. Its function is as a formulation component for lipid nanoparticles (LNPs). The ionizable cationic lipidoid facilitates the encapsulation and delivery of nucleic acids and other therapeutic payloads. Its ionizable nature allows for pH-dependent charge switching, which is important for endosomal escape and efficient cytosolic delivery. The disulfide bonds in the tails are designed to be biodegradable, enhancing the safety profile of the LNP formulation.
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| ln Vitro |
In vitro, 306-O12B-3 has been shown to effectively deliver ASOs to cells. The lipidoid forms LNPs that encapsulate ASOs and facilitate their cellular uptake and intracellular release. Its ionizable properties enable efficient endosomal escape, ensuring that the delivered payload reaches its intracellular target. The compound's in vitro delivery efficiency has been demonstrated in various cell culture models. Cytotoxicity of 306-O12B-3-containing LNPs is typically evaluated to ensure formulation safety.
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| ln Vivo |
In vivo, 306-O12B-3 has been used to deliver ASOs and small molecule drugs. The compound is used to transport small molecule drugs across the blood-brain barrier (BBB), suggesting potential applications in treating central nervous system disorders. LNPs formulated with 306-O12B-3 have demonstrated in vivo delivery efficacy in animal models. The biodegradable disulfide bonds in the lipidoid tails contribute to the overall safety and tolerability of the formulation.
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| Enzyme Assay |
In vitro assays for 306-O12B-3 primarily involve characterization of LNP formulations. LNPs are prepared by mixing the lipidoid with helper lipids, cholesterol, and the payload (ASO or drug). Particle size and polydispersity are measured by dynamic light scattering (DLS). Encapsulation efficiency is determined by gel retardation assay or fluorescence-based methods. Cellular uptake is assessed using fluorescently labeled payloads and flow cytometry or confocal microscopy. Endosomal escape is evaluated using colocalization studies with endosomal markers.
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| Cell Assay |
In vitro cellular assays for 306-O12B-3 involve treating cells with LNP-formulated payloads. The delivery efficiency of ASOs is assessed by measuring target gene knockdown using qRT-PCR or Western blotting. For small molecule drug delivery, efficacy is evaluated based on the pharmacological effect of the drug. Cytotoxicity is assessed using MTT or LDH release assays. The compound's effects on cell viability and function are evaluated to ensure formulation safety. These assays are performed using appropriate cell lines relevant to the disease model.
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| Animal Protocol |
In vivo animal studies for 306-O12B-3 involve administration of LNP-formulated payloads to rodent models. For ASO delivery, target gene knockdown is assessed in relevant tissues by qRT-PCR or Western blotting. For drug delivery across the BBB, biodistribution studies measure drug concentrations in the brain and other tissues. Therapeutic efficacy is evaluated in appropriate disease models. Safety and tolerability are assessed through monitoring of body weight, clinical signs, and histopathological examination of major organs.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 306-O12B-3 itself are not typically reported, as it is a formulation component rather than an active pharmaceutical ingredient. The pharmacokinetics of 306-O12B-3-containing LNPs depend on the overall formulation characteristics including particle size, surface charge, and PEGylation. LNPs generally distribute to the liver, spleen, and other organs of the reticuloendothelial system. The biodegradable disulfide bonds in 306-O12B-3 are designed to facilitate clearance and reduce accumulation.
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| Toxicity/Toxicokinetics |
306-O12B-3 is designed to be biodegradable, which contributes to its safety profile. The compound's disulfide bonds are expected to be cleaved in the reducing environment of cells, facilitating breakdown and clearance. Cytotoxicity of 306-O12B-3-containing LNPs is typically low at effective concentrations. However, comprehensive toxicological assessments have not been widely reported. The compound is intended for research use only and not for human therapeutic applications. Standard toxicological evaluations would include acute and repeat-dose toxicity studies in animal models.
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| References | |
| Additional Infomation |
306-O12B-3 is a research lipidoid used for the formulation of lipid nanoparticles (LNPs) for nucleic acid and drug delivery. It can effectively deliver ASOs in vitro and in vivo. The compound is used to transport small molecule drugs across the blood-brain barrier (BBB). Its ionizable cationic nature and biodegradable disulfide bonds make it a valuable tool for LNP formulation development. 306-O12B-3 is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C46H91N3O6S6
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| Molecular Weight |
974.62
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| Appearance |
Colorless to light yellow liquid
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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 :~3.33 mg/mL (~3.42 mM; with sonication (<60°C))
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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 | 1.0260 mL | 5.1302 mL | 10.2604 mL | |
| 5 mM | 0.2052 mL | 1.0260 mL | 2.0521 mL | |
| 10 mM | 0.1026 mL | 0.5130 mL | 1.0260 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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