| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Inclisiran sodium targets PCSK9 (proprotein convertase subtilisin/kexin type 9), a protein that promotes the degradation of LDL receptors. As an siRNA, it inhibits the transcription of PCSK9 through RNA interference, reducing hepatic synthesis of PCSK9. The GalNAc conjugation enables targeted delivery to hepatocytes via the asialoglycoprotein receptor. This mechanism leads to increased LDL receptor availability and reduced LDL cholesterol levels.
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| ln Vitro |
In vitro studies demonstrate that Inclisiran sodium functions as an siRNA that inhibits PCSK9 transcription through RNA interference. The GalNAc conjugation enables targeted delivery to hepatocytes. The compound reduces PCSK9 synthesis and increases LDL receptor availability. Detailed in vitro activity data, including IC50 values and knockdown efficiency, are not extensively documented in the available literature. The compound is intended for research use only.
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| ln Vivo |
In vivo activity of Inclisiran sodium has been demonstrated in preclinical and clinical studies. In transgenic mice expressing human PCSK9, the siRNA effectively silenced the human PCSK9 transcript and resulted in significant reduction of PCSK9 levels. Clinical studies have shown that Inclisiran sodium 100, 200, and 300 mg doses demonstrated clinically meaningful and statistically significant LDL-C and PCSK9 reductions. The compound is used for research of cardiovascular disease.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Inclisiran sodium is not applicable, as the compound is an siRNA that functions through RNA interference rather than enzyme inhibition. However, receptor binding assays may be performed to assess the interaction of the GalNAc moiety with the asialoglycoprotein receptor on hepatocytes. Binding affinity can be measured using surface plasmon resonance or cell-based uptake assays with fluorescently labeled siRNA.
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| Cell Assay |
In vitro cell-based assays for Inclisiran sodium are conducted using hepatocyte cell lines such as HepG2 cells. Cells are treated with the compound at various concentrations, and PCSK9 mRNA levels are measured by qPCR to assess knockdown efficiency. PCSK9 protein levels are measured by ELISA or Western blot. LDL receptor levels are assessed to confirm the functional effect. Cytotoxicity is evaluated using standard cell viability assays.
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| Animal Protocol |
In vivo animal studies for Inclisiran sodium have been conducted using transgenic mice expressing human PCSK9. Animals were administered the compound via subcutaneous injection, and PCSK9 transcript silencing and protein reduction were measured. Pharmacokinetic parameters were determined from plasma samples. The compound demonstrated potency in silencing human PCSK9 transcript and significant reduction of PCSK9 levels.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Inclisiran sodium include a mean terminal elimination half-life of approximately 9.6 hours. Tmax at the 300 mg dose was four hours. The compound does not accumulate with multiple dosing. Approximately 16% of the compound is cleared through the kidney. The plasma half-life ranges from 3.6 to 13.2 hours across different studies. The majority of plasma elimination is attributed to hepatic uptake.
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| Toxicity/Toxicokinetics |
Toxicity information for Inclisiran sodium is limited in the search results. As a research-use compound, standard safety precautions for handling should be followed. The compound is designated for research use only and is not for human therapeutic applications. Clinical studies have evaluated safety in patients, but detailed toxicity data are not available from the search results.
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| References | |
| Additional Infomation |
Inclisiran sodium (ALN-PCSsc sodium) is a GalNAc-conjugated siRNA that inhibits PCSK9 transcription. It reduces hepatic PCSK9 synthesis and is used for research of cardiovascular disease. The compound has a half-life of approximately 9.6 hours. It is intended for research use only.
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| Molecular Formula |
C529H663F12N176NA44O316P43S6
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| Molecular Weight |
17306.68
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| Appearance |
White to off-white solid powder
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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, 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) |
Typically soluble in DMSO (e.g. 10 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 | 0.0578 mL | 0.2889 mL | 0.5778 mL | |
| 5 mM | 0.0116 mL | 0.0578 mL | 0.1156 mL | |
| 10 mM | 0.0058 mL | 0.0289 mL | 0.0578 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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