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5A2-SC8

Cat No.:V50567 Purity: ≥98%
5A2-SC8 is a degradable lipid compound (ester-based dendritic molecule) for small RNA delivery.
5A2-SC8
5A2-SC8 Chemical Structure CAS No.: 1857341-90-2
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
100mg
1g
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Product Description
5A2-SC8 is a degradable lipid compound (ester-based dendritic molecule) for small RNA delivery.
5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. It is a degradable lipid compound (ester-based dendritic molecule) for small RNA delivery. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models. The CAS number is 1857341-90-2, with a molecular formula of C₉₃H₁₇₃N₅O₂₀S₅ and a molecular weight of 1841.72.
Biological Activity I Assay Protocols (From Reference)
Targets
5A2-SC8 targets the delivery of small RNAs (siRNA, miRNA) to tumor cells. It is an ionizable amino lipid used in lipid nanoparticles (LNPs) for RNA delivery. The ApoE protein corona adsorbs on the surface of 5A2-SC8 LNPs, binds to LDL-R on the surface of hepatocytes, and undergoes receptor-mediated endocytosis.
ln Vitro
In vitro, 5A2-SC8 is used as an ionizable amino lipid in LNPs for small RNA delivery. It shows high delivery potential. The ApoE protein corona adsorbs on the surface of 5A2-SC8 LNPs, binds to LDL-R on hepatocytes, and undergoes receptor-mediated endocytosis. It enables efficient delivery of siRNA and miRNA into tumor cells.
ln Vivo
In vivo, 5A2-SC8 (75 mg/kg; i.v.; single-dose) is well tolerated and does not affect survival in mice with chronic aggressive hepatocellular carcinoma. 5A2-SC8 (0.5 mg/kg; i.v.; single-dose) can pass the first barrier of Kupffer cells in the liver and be internalized into hepatocytes. It is used for efficient delivery of small RNAs such as siRNA and miRNA into tumor cells.
Enzyme Assay
There are no in vitro enzyme/receptor binding assays for 5A2-SC8 as it is a lipid for RNA delivery, not an enzyme inhibitor. Its function is assessed by its ability to deliver RNA into cells.
Cell Assay
In vitro cell-based assays for 5A2-SC8 involve formulating the lipid into LNPs with small RNAs and treating cells with the LNPs. RNA delivery efficiency is assessed by measuring the knockdown of target genes (for siRNA) or expression of reporter genes (for mRNA). Cell viability and toxicity are also evaluated.
Animal Protocol
In vivo animal studies for 5A2-SC8 involve administering 5A2-SC8 LNPs containing small RNAs to mice via intravenous injection. RNA delivery to the liver and tumor tissues is assessed. Therapeutic outcomes in cancer models are evaluated. Survival and toxicity are monitored.
ADME/Pharmacokinetics
Pharmacokinetic properties of 5A2-SC8 are not extensively detailed in the available literature. The compound is soluble in DMSO: 100 mg/mL (54.30 mM; Need ultrasonic). For storage, powder should be kept at -20°C, protect from light, stored under nitrogen; in solvent at -80°C for 6 months or -20°C for 1 month (protect from light, stored under nitrogen).
Toxicity/Toxicokinetics
No specific toxicity data for 5A2-SC8 are available in the provided literature. It shows low in vivo toxicity. 5A2-SC8 (75 mg/kg; i.v.; single-dose) is well tolerated in mice. The compound is for research use only.
References
:Modular degradable dendrimers enable small RNAs to extend survival in an aggressive liver cancer model.Proc Natl Acad Sci U S A. 2016;113(3):520-525.
Additional Infomation
5A2-SC8 is an ionizable amino lipid for RNA delivery. It shows high delivery potential and low in vivo toxicity. It is used for efficient delivery of siRNA and miRNA into tumor cells. Its CAS number is 1857341-90-2.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C93H173N5O20S5
Molecular Weight
1841.72
Exact Mass
1840.127
CAS #
1857341-90-2
PubChem CID
129092701
Appearance
Colorless to light yellow ointment
LogP
20.9
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
30
Rotatable Bond Count
102
Heavy Atom Count
123
Complexity
2340
Defined Atom Stereocenter Count
0
SMILES
CCCCCCCCSCC(C)C(=O)OCCOC(=O)CCN(CCC(=O)OCCOC(=O)C(C)CSCCCCCCCC)CCNCCN(CCC(=O)OCCOC(=O)C(C)CSCCCCCCCC)CCNCCN(CCC(=O)OCCOC(=O)C(C)CSCCCCCCCC)CCC(=O)OCCOC(=O)C(C)CSCCCCCCCC
InChi Key
BYWPQQOQVPVCTC-UHFFFAOYSA-N
InChi Code
InChI=1S/C93H173N5O20S5/c1-11-16-21-26-31-36-69-119-74-79(6)89(104)114-64-59-109-84(99)41-50-96(51-42-85(100)110-60-65-115-90(105)80(7)75-120-70-37-32-27-22-17-12-2)55-46-94-48-57-98(54-45-88(103)113-63-68-118-93(108)83(10)78-123-73-40-35-30-25-20-15-5)58-49-95-47-56-97(52-43-86(101)111-61-66-116-91(106)81(8)76-121-71-38-33-28-23-18-13-3)53-44-87(102)112-62-67-117-92(107)82(9)77-122-72-39-34-29-24-19-14-4/h79-83,94-95H,11-78H2,1-10H3
Chemical Name
2-[3-[2-[2-[2-[2-[bis[3-[2-(2-methyl-3-octylsulfanylpropanoyl)oxyethoxy]-3-oxopropyl]amino]ethylamino]ethyl-[3-[2-(2-methyl-3-octylsulfanylpropanoyl)oxyethoxy]-3-oxopropyl]amino]ethylamino]ethyl-[3-[2-(2-methyl-3-octylsulfanylpropanoyl)oxyethoxy]-3-oxopropyl]amino]propanoyloxy]ethyl 2-methyl-3-octylsulfanylpropanoate
HS Tariff Code
2934.99.9001
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 and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~54.30 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.5430 mL 2.7149 mL 5.4297 mL
5 mM 0.1086 mL 0.5430 mL 1.0859 mL
10 mM 0.0543 mL 0.2715 mL 0.5430 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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