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| Targets |
Toll-like receptor 3 (TLR3), TLR7/8 (in some contexts), RIG-I, and MDA5. Poly(I:C) is recognized by TLR3 in endosomes and by RIG-I and MDA5 in the cytoplasm. The potassium salt form of poly(I:C) is believed to be preferentially recognized by TLR7/8 in certain immune cell types. Binding to these receptors triggers the activation of downstream signaling cascades, including the NF-kappaB and IRF3 pathways, leading to the production of type I interferons (IFN-alpha/beta), pro-inflammatory cytokines (IL-6, TNF-alpha), and chemokines, thereby mimicking a viral infection and promoting adaptive immune responses.
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| ln Vitro |
In vitro, polycytidylic acid potassium is used to stimulate cultured immune cells, such as dendritic cells, macrophages, and lymphocytes. At concentrations ranging from 0.1 to 100 microg/mL, it induces the expression of type I interferons and pro-inflammatory cytokines, upregulates co-stimulatory molecules (CD80, CD86), and enhances antigen presentation. It also activates natural killer (NK) cells, promoting cytotoxicity and IFN-gamma secretion. In tumor cell lines, poly(I:C) has been shown to induce apoptosis and inhibit proliferation through activation of the intrinsic apoptotic pathway. These activities make it a valuable tool for studying innate immunity, vaccine adjuvants, and antitumor immune responses.
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| ln Vivo |
In vivo, polycytidylic acid potassium is administered to mice and other animal models to simulate viral infections. Intraperitoneal or intravenous injection (typically 0.5-10 mg/kg) induces a systemic inflammatory response characterized by elevated serum levels of IFN-alpha, IFN-beta, IL-6, and TNF-alpha. It also triggers fever, malaise, and leukocyte infiltration in various tissues. In tumor-bearing mice, poly(I:C) exhibits antitumor effects by promoting the infiltration of activated immune cells into the tumor microenvironment and enhancing tumor antigen cross-presentation. Additionally, it is used as a vaccine adjuvant to boost antibody and T-cell responses against co-administered antigens.
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| Enzyme Assay |
For in vitro assays without cells, poly(I:C) is typically dissolved directly in sterile, nuclease-free water, PBS, or cell culture medium at a concentration of 1 mg/mL. The solution is heated to 65-70degC for 5-10 minutes, then cooled slowly to room temperature to ensure proper annealing of the double-stranded structure. The annealed poly(I:C) solution is then filtered through a 0.22 microm filter for sterilization. Binding to TLR3 can be assessed using surface plasmon resonance (SPR) or ELISA-based binding assays with recombinant TLR3-Fc fusion protein immobilized on a sensor chip or plate. Alternatively, poly(I:C) can be labeled with biotin or a fluorescent tag to study its interaction with purified RIG-I or MDA5 proteins in pull-down assays.
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| Cell Assay |
For cell stimulation, polycytidylic acid potassium is prepared as a 1 mg/mL stock solution in sterile, nuclease-free water or PBS. The stock is heated to 65-70degC for 5-10 minutes and annealed by slow cooling. This stock can be stored at -20degC for up to 6 months. For experimental use, the stock is diluted to working concentrations of 0.1-100 microg/mL in serum-free or complete culture medium. Adherent cells are seeded at 1×10⁵-5×10⁵ cells/well in 24-well plates 24 hours before treatment. Cells are washed with PBS, then treated with poly(I:C) for 6-48 hours. For transfection of poly(I:C) into the cytoplasm to activate RIG-I/MDA5, lipofectamine or other cationic lipid reagents are used to deliver 0.1-10 microg/mL poly(I:C) into cells. Cells are harvested at various time points for RNA extraction, protein lysate preparation, or flow cytometry analysis.
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| Animal Protocol |
A typical in vivo protocol involves preparing polycytidylic acid potassium in sterile, endotoxin-free PBS at a concentration of 0.5-2 mg/mL. For intravenous (tail vein) or intraperitoneal injection, mice receive a single dose of 1-20 mg/kg body weight. For intratumoral injection, a volume of 25-100 microL (1-5 mg/kg equivalent) is injected directly into the tumor mass. Blood samples are collected via retro-orbital or cardiac puncture at 2, 4, 8, 12, 24, and 48 hours post-injection to measure cytokine levels by ELISA. For tissue analysis, mice are euthanized, and organs (spleen, liver, lung, tumor) are harvested for histological analysis, RNA extraction, or protein analysis. For vaccine adjuvant studies, poly(I:C) is co-administered with antigen in PBS and administered subcutaneously or intramuscularly on days 0, 7, and 14.
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| ADME/Pharmacokinetics |
Poly(I:C) exhibits rapid clearance from the circulation following intravenous administration, with an initial half-life of approximately 2-10 minutes and a terminal half-life of 20-40 minutes. It is rapidly taken up by the liver (via Kupffer cells), spleen, and lungs, where it interacts with TLR3-expressing immune cells. Peak serum concentrations of pro-inflammatory cytokines (e.g., IFN-alpha, IL-6, TNF-alpha) occur 2-4 hours post-injection, returning to baseline by 24-48 hours. Poly(I:C) is degraded by serum nucleases and phagocytic cells, and its metabolites are excreted in the urine. The bioavailability after intraperitoneal administration is moderate (~30-50%), with a delayed peak cytokine response compared to intravenous administration. For intratumoral administration, poly(I:C) remains localized within the tumor for up to 48-72 hours.
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| Toxicity/Toxicokinetics |
Toxicological studies in mice show that poly(I:C) at low to moderate doses (1-10 mg/kg) induces a self-limited inflammatory response with minimal organ toxicity. Higher doses (>20 mg/kg) can cause severe systemic inflammation, leading to cytokine storm, multiple organ dysfunction (particularly liver and kidney), and mortality. Common adverse effects include transient fever, reduced activity, weight loss, and piloerection. Histological examination reveals mild to moderate inflammation in the liver and spleen, characterized by mononuclear cell infiltration. Chronic administration studies are limited. The compound is for research use only and is not approved for human therapeutic use. Due to its potent immune-stimulating activity, it should be handled with care to avoid accidental exposure.
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| References | |
| Additional Infomation |
Polycytidylic acid potassium is a research-grade chemical not approved for clinical use. It is a white to off-white powder with a purity of ≥85% (typically 98% by HPLC). It is soluble in water, PBS, and cell culture media, with a solubility of approximately 10-20 mg/mL. The compound should be stored at -20degC for long-term storage, protected from light and moisture. Stock solutions can be stored at -20degC for up to 6 months, but repeated freeze-thaw cycles should be avoided. It is a common tool in immune system research, especially for studying antiviral immune responses, vaccine adjuvants, and cancer immunotherapy. Synonyms include poly(I:C) potassium salt, polyinosinic-polycytidylic acid potassium salt, and poly(C9H13N3O8P).xK. It is also used experimentally to simulate viral infections in vivo.
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| Molecular Formula |
C9H12K2N3O8P
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|---|---|
| Molecular Weight |
399.377244949341
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| Exact Mass |
361.007
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| CAS # |
26936-40-3
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| PubChem CID |
71495275
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
520
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| Defined Atom Stereocenter Count |
4
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| SMILES |
[K+].[K+].P(=O)([O-])([O-])OCC1C(C(C(N2C(N=C(C=C2)N)=O)O1)O)O
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| InChi Key |
KJFHSFLOUJGHLS-WFIJOQBCSA-L
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| InChi Code |
InChI=1S/C9H14N3O8P.2K/c10-5-1-2-12(9(15)11-5)8-7(14)6(13)4(20-8)3-19-21(16,17)18;;/h1-2,4,6-8,13-14H,3H2,(H2,10,11,15)(H2,16,17,18);;/q;2*+1/p-2/t4-,6-,7-,8-;;/m1../s1
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| Chemical Name |
dipotassium;[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5039 mL | 12.5194 mL | 25.0388 mL | |
| 5 mM | 0.5008 mL | 2.5039 mL | 5.0078 mL | |
| 10 mM | 0.2504 mL | 1.2519 mL | 2.5039 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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