cKK-E12 |
رقم الكتالوجGC52025
One-Click Copy Product Info
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CKK-E12 عبارة عن دهون مؤينة مع دهون أخرى تشكل الجسيمات النانوية الدهنية التي تستخدم لتقديم العلاجات القائمة على الحمض النووي الريبي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432494-65-9
Sample solution is provided at 25 µL, 10mM.
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cKK-E12 is an ionizable lipid that can be used to form lipid nanoparticles (LNP) for efficient delivery of siRNA and mRNA[1]. LNP formed with cKK-E12 exhibit high surface binding affinity for endogenous apolipoprotein E (ApoE), demonstrating strong tropism for hepatocytes[2]. cKK-E12 is commonly applied in targeted gene delivery and therapy, vaccine development, molecular imaging, and related fields[3,4].
In vitro, treatment of RAW 264.7 macrophages with cKK-E12 LNP (400ng/mL) for 6h significantly upregulates the expression of pro-inflammatory cytokines IL-6, TNF-α, IL-1α, IFN-β, and the chemokine MCP-1. Furthermore, treatment with cKK-E12 LNP (400ng/mL) for 24h markedly increases the proportions of apoptotic, necrotic, and pyroptotic cells[5].
In vivo, administration of Cy5-labeled mRNA-loaded cKK-E12 LNP (0.75mg/kg) via tail vein injection in C57BL/6 mice results in predominant accumulation in the liver (>60%) within 1h, followed by the spleen, lungs, and kidneys[6]. Intravenous injection of trastuzumab mRNA-loaded cKK-E12 LNP (0.5, 1, and 2mg/kg) in C57BL/6 mice leads to a dose-dependent increase in serum trastuzumab levels after 24h, reaching approximately 40µg/mL at the 2mg/kg dose[7].
References:
[1] ZENG Y, ESCALONA-RAYO O, KNOL R, et al. Lipid nanoparticle-based mRNA candidates elicit potent T cell responses[J]. Biomaterials Science, 2023, 11(3): 964-974.
[2] DONG Y, LOVE K T, DORKIN J R, et al. Lipopeptide nanoparticles for potent and selective siRNA delivery in rodents and nonhuman primates[J]. Proceedings of the National Academy of Sciences, 2014, 111(11): 3955-3960.
[3] FENTON O S, KAUFFMAN K J, MCCLELLAN R L, et al. Bioinspired alkenyl amino alcohol ionizable lipid materials for highly potent in vivo mRNA delivery[J]. Advanced Materials (Deerfield Beach, Fla.), 2016, 28(15): 2939.
[4] GORDON A, LI B, WITTEN J, et al. Inhalable dry powders for lung mRNA delivery[J]. Advanced Healthcare Materials, 2024, 13(29): 2400509.
[5] OMO-LAMAI S, WANG Y, PATEL M N, et al. Lipid nanoparticle-associated inflammation is triggered by sensing of endosomal damage: engineering endosomal escape without side effects[J]. bioRxiv, 2024: 2024.04.16.589801.
[6] MELAMED J R, HAJJ K A, CHAUDHARY N, et al. Lipid nanoparticle chemistry determines how nucleoside base modifications alter mRNA delivery[J]. Journal of Controlled Release, 2022, 341: 206-214.
[7] RYBAKOVA Y, KOWALSKI P S, HUANG Y, et al. mRNA delivery for therapeutic anti-HER2 antibody expression in vivo[J]. Molecular Therapy, 2019, 27(8): 1415-1423.
| Cell experiment [1]: | |
Cell lines | RAW 264.7 macrophages |
Preparation Method | RAW 264.7 macrophages were treated with cKK-E12 LNP at a dose of 400ng/mL of mRNA for 6h, and the concentrations of pro-inflammatory cytokines (IL-6, TNF-α, IL-1α, IFN-β) and chemokine MCP-1 in the supernatant were measured using a multiplex cytokine assay. |
Reaction Conditions | 400ng/mL; 6h |
Applications | cKK-E12 LNP treatment significantly upregulated the expression of pro-inflammatory cytokines IL-6, TNF-α, IL-1α, IFN-β and chemokine MCP-1. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice were injected via tail vein with cKK-E12 LNP encapsulating Cy5-labeled mRNA (dose 0.75mg/kg). 1h post-injection, mice were sacrificed, and major organs (liver, spleen, lungs, and kidneys) were harvested and subjected to ex vivo fluorescence imaging using an IVIS imaging system (Ex/Em: 649/670nm). Percent biodistribution was calculated for each organ based on total radiant efficiency analyzed via region of interest using Living Image software. |
Dosage form | 0.75mg/kg; i.v. |
Applications | Most cKK-E12 LNP accumulated in the liver (>60%) and, to a lesser extent, the spleen, kidneys, and lungs. |
References: | |
| Cas No. | 1432494-65-9 | SDF | |
| Canonical SMILES | O=C1NC(CCCCN(CC(CCCCCCCCCC)O)CC(CCCCCCCCCC)O)C(NC1CCCCN(CC(CCCCCCCCCC)O)CC(CCCCCCCCCC)O)=O | ||
| Formula | C60H120N4O6 | M.Wt | 993.6 |
| الذوبان | DMSO : 50 mg/mL (50.32 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0064 mL | 5.0322 mL | 10.0644 mL |
| 5 mM | 201.3 μL | 1.0064 mL | 2.0129 mL |
| 10 mM | 100.6 μL | 503.2 μL | 1.0064 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A liquid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)