| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
YSK-05 does not have a classical protein target. Its primary target is the endosomal membrane. As a pH-sensitive cationic lipid, it facilitates the escape of nucleic acid cargo from endosomes into the cytoplasm, a major barrier to effective gene delivery.
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|---|---|
| ln Vitro |
By encouraging MEND's endosomal escape, YSK 05 improves the effectiveness of siRNA transport to the cytoplasm and gene silencing [1].
YSK-05-MEND, the lipid nanoparticle formulation containing YSK-05, demonstrates significantly good gene silencing activity and hemolytic activity in vitro. It effectively overcomes the suppression of endosomal escape caused by polyethylene glycol (PEG) modification, enhancing siRNA delivery. |
| ln Vivo |
YSK-05 effectively enhances siRNA delivery in vivo. In animal models, YSK-05 formulated lipid nanoparticles delivered siRNA to hepatocytes and demonstrated significant gene silencing after intravenous administration.
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| Enzyme Assay |
The pKa of YSK-05 (apparent pKa ~6.5) is determined to characterize its pH-sensitive properties. Hemolytic activity is assessed by measuring hemoglobin release from red blood cells at various pH levels. Endosomal escape is evaluated in cell-based assays using fluorescently labeled siRNA.
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| Cell Assay |
HeLa or other cell lines are transfected with siRNA/YSK-05 lipoplexes. Gene silencing efficiency is quantified by measuring knockdown of a target gene (e.g., luciferase or a housekeeping gene) via qPCR or Western blot. Intracellular trafficking is visualized using confocal microscopy.
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| Animal Protocol |
In vivo protocols involve intravenous injection of siRNA-loaded YSK-05 lipid nanoparticles into mice (e.g., C57BL/6). After a specified time (e.g., 24-72 hours), tissues (liver, spleen) are harvested, and target gene expression is measured to assess gene silencing efficacy.
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| ADME/Pharmacokinetics |
PK properties are characteristic of lipid nanoparticles. The siRNA cargo is protected from degradation and has an extended circulation time. YSK-05 itself is expected to be metabolized and cleared like other lipid components. Comprehensive ADME data is not publicly detailed.
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| Toxicity/Toxicokinetics |
Toxicological assessment includes monitoring for hepatotoxicity via serum ALT/AST levels after administration. Histological analysis of major organs (liver, spleen, kidneys) is performed to assess tissue damage. YSK-05-MEND was well-tolerated in animal studies.
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| References | |
| Additional Infomation |
YSK-05 is an ionizable amino lipid that has been used in combination with other lipids (DSPC, cholesterol, PEG-lipid) to formulate LNP systems for nucleic acid delivery. It is a research tool for non-viral gene therapy and is not an approved drug.
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| Molecular Formula |
C42H77NO2
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|---|---|
| Molecular Weight |
628.07
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| Exact Mass |
627.595
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| CAS # |
1318793-78-0
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| PubChem CID |
53339481
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| Appearance |
Colorless to light yellow liquid
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| LogP |
14.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
32
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| Heavy Atom Count |
45
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| Complexity |
664
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCC/C=C\C/C=C\CCCCCCCCOC1(CCN(CC1)C)OCCCCCCCC/C=C\C/C=C\CCCCC
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| InChi Key |
KURBRAZBXURPCJ-QYCRHRGJSA-N
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| InChi Code |
InChI=1S/C42H77NO2/c1-4-6-8-10-12-14-16-18-20-22-24-26-28-30-32-34-40-44-42(36-38-43(3)39-37-42)45-41-35-33-31-29-27-25-23-21-19-17-15-13-11-9-7-5-2/h12-15,18-21H,4-11,16-17,22-41H2,1-3H3/b14-12-,15-13-,20-18-,21-19-
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| Chemical Name |
1-methyl-4,4-bis[(9Z,12Z)-octadeca-9,12-dienoxy]piperidine
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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 : ~100 mg/mL (~159.22 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 | 1.5922 mL | 7.9609 mL | 15.9218 mL | |
| 5 mM | 0.3184 mL | 1.5922 mL | 3.1844 mL | |
| 10 mM | 0.1592 mL | 0.7961 mL | 1.5922 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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