| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Pam2CSK4 targets Toll-like receptor 2 (TLR2), a pattern recognition receptor that recognizes bacterial lipoproteins and lipopeptides. Unlike some other TLR2 ligands, Pam2CSK4 does not require TLR6 for signaling, making it a TLR6-independent TLR2 agonist. TLR2 activation triggers downstream MyD88-dependent signaling pathways leading to NF-κB activation and pro-inflammatory cytokine production.
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| ln Vitro |
Pam2CSK4 shows potent in vitro activity as a TLR2 agonist. It activates TLR2 signaling in various cell types, inducing the production of pro-inflammatory cytokines such as IL-6, IL-8, and TNF-α. The compound promotes platelet aggregation and increases platelet adhesion to collagen-coated surfaces, indicating its role in platelet activation and hemostasis. The EC₅₀ for TLR2 activation is in the low nanomolar range.
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| ln Vivo |
Pam2CSK4 demonstrates in vivo activity as an immunostimulatory agent. It is used in research models of bacterial infection and sepsis to study TLR2-mediated immune responses. The compound can be administered via various routes (intraperitoneal, intravenous, subcutaneous) to induce inflammatory responses and investigate the role of TLR2 in host defense and inflammatory diseases.
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| Enzyme Assay |
Non-cell-based binding assays for Pam2CSK4 typically involve surface plasmon resonance (SPR) or ELISA to measure TLR2 binding affinity. A typical protocol includes: immobilizing recombinant TLR2 protein on a sensor chip or plate, flowing Pam2CSK4 at various concentrations, and measuring binding response. Competition assays with labeled Pam2CSK4 can be used to determine the affinity of other TLR2 ligands.
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| Cell Assay |
Cellular assays with Pam2CSK4 typically involve TLR2-expressing cell lines or primary immune cells. A representative protocol includes: culturing HEK293 cells transfected with TLR2 or primary human monocytes/macrophages, treating with Pam2CSK4 at various concentrations (0.01–10 μg/mL) for 4–24 hours, measuring cytokine production by ELISA or qRT-PCR, and assessing NF-κB activation by reporter gene assay or Western blot.
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| Animal Protocol |
In vivo animal studies with Pam2CSK4 typically involve mouse models of inflammation or infection. A representative protocol includes: administering Pam2CSK4 via intraperitoneal (1–10 mg/kg) or intravenous injection, monitoring inflammatory responses (cytokine levels, body temperature, clinical signs), collecting blood and tissues for analysis, and assessing the role of TLR2 in host defense by comparing wild-type and TLR2-knockout mice.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Pam2CSK4 have not been extensively reported. As a lipopeptide, it is expected to have rapid clearance from circulation, binding to plasma proteins and cell membranes, and limited oral bioavailability. The compound is typically administered via injection in research studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Pam2CSK4 are limited as it is a research-use compound. At high doses, TLR2 activation may induce excessive inflammatory responses leading to systemic inflammation and tissue damage. Standard safety precautions should be followed when handling the compound. The TFA salt form is used to enhance solubility and stability.
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| References |
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| Additional Infomation |
Pam2CSK4 (TFA) is a valuable research tool for studying TLR2-mediated immune responses, bacterial lipoprotein recognition, and platelet activation. As a TLR6-independent TLR2 agonist, it allows for dissection of TLR2 signaling pathways independent of TLR6 heterodimerization. The compound is widely used in immunology research to investigate host-pathogen interactions, inflammatory diseases, and vaccine adjuvant development.
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| Molecular Formula |
C65H126N10O12S.XC2HF3O2
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| Molecular Weight |
1271.82 (free base)
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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 (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)
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| Solubility (In Vitro) |
H2O :~100 mg/mL (with sonication)
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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.) |
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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