DLin-KC2-DMA [1190197-97-7]

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DLin-KC2-DMA is an ionisable cationic lipid (pKa≈6) that is virtually non-toxic to antigen presenting cells (APCs). DLin-KC2-DMA produces significant siRNA-mediated gene silencing of GAPDH, when binds to lipid nanoparticles (LNP). DLin-KC2-DMA can be used in siRNA delivery studies.

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DLin-KC2-DMA Estructura química

DLin-KC2-DMA Estructura química

No. CAS : 1190197-97-7

This product is a controlled substance and not for sale in your territory.

Based on 4 publication(s) in Google Scholar

Descripciòn

DLin-KC2-DMA is an ionisable cationic lipid (pKa≈6) that is virtually non-toxic to antigen presenting cells (APCs). DLin-KC2-DMA produces significant siRNA-mediated gene silencing of GAPDH, when binds to lipid nanoparticles (LNP). DLin-KC2-DMA can be used in siRNA delivery studies[1][2].

In Vitro

DLin-KC2-DMA (1, 5 μg; 72 h) effectively produces a significant siRNA-mediated GAPDH gene silencing in both macrophages and dendritic cells[1].
DLin-KC2-DMA (24 h) exhibits high uptake into macrophages and dendritic cells[1].
DLin-KC2-DMA efficiently promotes release of encapsulated siRNA into the cytosol following uptake via the endocytotic pathway[1].
DLin-KC2-DMA displays almost no toxicity in primary APCs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Macrophages, dendritic cells
Concentration: 5 μg/mL (DLin-KC2-DMA contained-LNPs)
Incubation Time: 72 h
Result: Displayed almost no toxicity.

Western Blot Analysis[1]

Cell Line: Macrophages, dendritic cells
Concentration: 1, 5 μg
Incubation Time: 72 h
Result: Exhibited significant GAPDH silencing of more than 60% at 1 μg and of 80% at 5 μg in macrophages.
Significantly reduced GAPDH protein and exhibited the silencing effects of 83% at 5 μg.
In Vivo

DLin-KC2-DMA contained-LNP siRNA systems (5 mg/kg; i.v.; single) effectively silences target genes in APcs in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Naive C57BL/6 mice[1].
Dosage: 3 or 5 mg/kg (DLin-KC2-DMA contained-LNPs)
Administration: Intravenous injection; single.
Result: Significantly reduced GAPDH production in peritoneal cavity macrophages and dendritic cells and in the spleen-derived APCs when at 5 mg/kg.
Peso molecular

642.09

Fòrmula

C43H79NO2

No. CAS

1190197-97-7

Appearance

Liquid

Color

Colorless to light yellow

SMILES

CCCCC/C=C\C/C=C\CCCCCCCCC1(CCCCCCCC/C=C\C/C=C\CCCCC)OC(CCN(C)C)CO1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-20°C, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvente y solubilidad
In Vitro: 

Ethanol : 100 mg/mL (155.74 mM; Need ultrasonic)

DMSO : 100 mg/mL (155.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5574 mL 7.7871 mL 15.5741 mL
5 mM 0.3115 mL 1.5574 mL 3.1148 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: ≥98.0%

Referencias
  • [1]. Basha G, et al. Influence of cationic lipid composition on gene silencing properties of lipid nanoparticle formulations of siRNA in antigen-presenting cells. Mol Ther. 2011 Dec;19(12):2186-200.  [Content Brief]

    [2]. Miller AD, et al. Delivery of RNAi therapeutics: work in progress. Expert Rev Med Devices. 2013 Nov;10(6):781-811.  [Content Brief]

  • [1]. Basha G, et al. Influence of cationic lipid composition on gene silencing properties of lipid nanoparticle formulations of siRNA in antigen-presenting cells. Mol Ther. 2011 Dec;19(12):2186-200.

    [2]. Miller AD, et al. Delivery of RNAi therapeutics: work in progress. Expert Rev Med Devices. 2013 Nov;10(6):781-811.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.5574 mL 7.7871 mL 15.5741 mL 38.9354 mL
5 mM 0.3115 mL 1.5574 mL 3.1148 mL 7.7871 mL
10 mM 0.1557 mL 0.7787 mL 1.5574 mL 3.8935 mL
15 mM 0.1038 mL 0.5191 mL 1.0383 mL 2.5957 mL
20 mM 0.0779 mL 0.3894 mL 0.7787 mL 1.9468 mL
25 mM 0.0623 mL 0.3115 mL 0.6230 mL 1.5574 mL
30 mM 0.0519 mL 0.2596 mL 0.5191 mL 1.2978 mL
40 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9734 mL
50 mM 0.0311 mL 0.1557 mL 0.3115 mL 0.7787 mL
60 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6489 mL
80 mM 0.0195 mL 0.0973 mL 0.1947 mL 0.4867 mL
100 mM 0.0156 mL 0.0779 mL 0.1557 mL 0.3894 mL
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DLin-KC2-DMA Related Classifications

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Keywords:

DLin-KC2-DMA1190197-97-7LiposomesiRNALNPmacrophagesdendritic cellsgene silenceInhibitorinhibitorinhibit

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