| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
RS 09 TFA targets the Toll-like receptor 4 (TLR4), a key pattern recognition receptor (PRR) in the innate immune system. TLR4 recognizes bacterial lipopolysaccharide (LPS) and triggers a signaling cascade leading to the production of pro-inflammatory cytokines. By acting as a synthetic TLR4 agonist, RS 09 activates this pathway. It is a peptide, which may offer different pharmacokinetic properties compared to the natural LPS ligand.
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| ln Vitro |
In vitro, RS 09 TFA induces the production of cytokines such as IL-6 and TNF-alpha through the activation of TLR4 signaling pathways. It can be used to stimulate immune cells in culture to study the mechanisms of inflammation and host defense against bacteria. The specific EC50 or IC50 values are not provided. It serves as a specific tool for stimulating the TLR4 pathway without the complexity of natural products like LPS.
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| ln Vivo |
In vivo, RS 09 TFA can be used as an immune-stimulating agent to study its effects on the immune system. It is a TLR4 agonist that can induce a systemic inflammatory response when administered in animal models. This makes it a valuable tool for studying sepsis, organ injury, and for evaluating the efficacy of anti-inflammatory drugs. It may also be investigated as a potential vaccine adjuvant to enhance immune responses to co-administered antigens.
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| Enzyme Assay |
A cell-free binding assay for RS 09 TFA can be performed using SPR to measure its interaction with the TLR4/MD2 complex. Recombinant human TLR4 and its co-receptor MD2 (CD14) are co-immobilized on a biosensor chip. Increasing concentrations of RS 09 TFA (1 nM - 10 uM) are flowed over the chip. The association (kon) and dissociation (koff) rates are measured, and the equilibrium dissociation constant (Kd) is calculated. This assay confirms direct binding of the peptide to the TLR4 receptor complex.
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| Cell Assay |
RS 09 TFA is used in cell-based assays to activate the TLR4 pathway. Human monocytic cell lines (e.g., THP-1) or primary human peripheral blood mononuclear cells (PBMCs) are seeded in 96-well plates. Cells are treated with varying concentrations of RS 09 TFA (0.1-100 ug/mL) for 4-24 h. The activation of the TLR4 signaling pathway is assessed by measuring the secretion of cytokines (e.g., TNF-alpha, IL-6, IL-1beta) in the cell culture supernatant using ELISA. The activation of the NF-kappaB pathway can be measured in reporter cells (e.g., HEK-Blue™ hTLR4 cells) by quantifying the expression of a secreted embryonic alkaline phosphatase (SEAP) reporter gene.
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| Animal Protocol |
RS 09 TFA can be tested in a mouse model of endotoxemia/sepsis. Male C57BL/6 mice (8-10 weeks, n=8 per group) are injected intraperitoneally (i.p.) with RS 09 TFA (1-10 mg/kg). Blood samples are collected at 2, 6, and 24 h post-injection. Serum levels of TNF-alpha, IL-6, and IL-1beta are measured by ELISA. To assess organ damage, mice are euthanized 6 h after treatment, and lung and liver tissues are collected for histopathological analysis (H&E staining) and measurement of myeloperoxidase (MPO) activity. This model is used to study the systemic inflammatory response.
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| ADME/Pharmacokinetics |
Detailed PK data for RS 09 TFA are not provided. As a peptide, its plasma half-life is expected to be short (minutes to hours). The TFA salt enhances solubility for injection. For in vivo studies, it is typically formulated in sterile PBS or saline. The powder should be stored at -20degC for up to 3 years. In solution, it is stable for 6 months at -80degC.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for RS 09 TFA are available. As a TLR4 agonist, its primary mechanism-based toxicity is the induction of a potent inflammatory response (cytokine storm), which can lead to septic shock, organ failure, and death if administered at high doses. Therefore, doses must be carefully titrated in animal studies. Standard safety precautions for handling immunostimulatory compounds should be followed.
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| References | |
| Additional Infomation |
RS 09 TFA is a research-grade peptide and is not approved for clinical use. It is a TLR4 agonist used as a tool to study innate immune activation and inflammation. It offers a synthetic alternative to LPS for research into sepsis, vaccine adjuvants, and anti-inflammatory therapeutics. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C33H50F3N9O11
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| Molecular Weight |
805.80
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| Related CAS # |
RS 09;1449566-36-2
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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) |
DMSO :≥ 100 mg/mL (~124.10 mM)
H2O :≥ 50 mg/mL (~62.05 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2410 mL | 6.2050 mL | 12.4100 mL | |
| 5 mM | 0.2482 mL | 1.2410 mL | 2.4820 mL | |
| 10 mM | 0.1241 mL | 0.6205 mL | 1.2410 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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