| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
The compound targets Toll-like receptor 4 (TLR4), a key pattern recognition receptor of the innate immune system that recognizes bacterial lipopolysaccharide (LPS). As a TLR4 agonist, RS-09 binds to TLR4 and activates the MyD88-dependent and TRIF-dependent signaling pathways, leading to NF-kappaB nuclear translocation and the induction of inflammatory cytokine secretion, thereby mimicking the immunostimulatory effects of LPS without its toxic components.
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| ln Vitro |
RS-09 promotes NF-kappaB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. It acts as a TLR4 agonist, stimulating the production of pro-inflammatory cytokines such as TNF-alpha, IL-6, and IL-1beta, as well as chemokines. This activity is comparable to the effects of LPS, but RS-09 is a defined synthetic peptide, offering improved purity, consistency, and safety profile compared to natural LPS preparations.
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| ln Vivo |
RS-09 acts as an adjuvant in vivo, enhancing antigen-specific antibody production in a vaccine setting. By activating TLR4 signaling, the peptide promotes the maturation of dendritic cells and the activation of B-cells and T-cells, leading to a robust adaptive immune response. When co-administered with antigens, RS-09 increases antibody titers and can also promote a Th1-biased immune response, making it a valuable adjuvant for vaccine research, particularly for infectious diseases and cancer immunotherapy.
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| Enzyme Assay |
RS-09 is a TLR4 agonist that binds to the TLR4/MD2 complex. Its binding and activation can be measured using a TLR4 reporter cell line. HEK293 cells stably transfected with human TLR4, MD2, CD14, and an NF-kappaB-driven luciferase reporter gene are seeded in 96-well plates. Varying concentrations of RS-09 (0.1-100 microM) are added to the cells, and after 4-6 hours of incubation, the cells are lysed, and luciferase activity is measured using a luminometer. The EC50 for TLR4 activation is calculated from the dose-response curve.
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| Cell Assay |
A cellular activation assay is performed using RAW264.7 murine macrophages or primary human peripheral blood mononuclear cells (PBMCs). Cells are seeded in 96-well plates and treated with varying concentrations of RS-09 (0.1-10 microg/mL) for 4-24 hours. After treatment, culture supernatants are collected, and the levels of pro-inflammatory cytokines (TNF-alpha, IL-6, IL-1beta) are measured by ELISA. Alternatively, cells are harvested and lysed for Western blot analysis of NF-kappaB nuclear translocation or phosphorylation of p38 MAPK, JNK, and IkappaBalpha.
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| Animal Protocol |
RS-09 acts as an adjuvant in vivo. In a typical vaccine study, female BALB/c or C57BL/6 mice are immunized subcutaneously or intramuscularly with a model antigen (e.g., ovalbumin (OVA) or a specific pathogen antigen) alone or in combination with RS-09 (e.g., 10-100 microg per mouse) as an adjuvant on days 0, 14, and 28. Blood samples are collected at various time points to measure antigen-specific antibody titers (IgG, IgG1, IgG2a) by ELISA. On day 35, mice are sacrificed, and splenocytes are isolated for T-cell proliferation assays and cytokine analysis (IFN-gamma, IL-4).
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| ADME/Pharmacokinetics |
Specific pharmacokinetic parameters for RS-09 are not detailed. As a synthetic peptide (MW ~691.78), it is not expected to be orally bioavailable. It is typically administered via subcutaneous, intramuscular, or intraperitoneal injection as part of a vaccine formulation. Its half-life in circulation may be short due to rapid degradation by proteases, which is acceptable for an adjuvant that needs to activate innate immunity locally at the injection site rather than systemically.
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| Toxicity/Toxicokinetics |
RS-09 is a synthetic TLR4 agonist peptide and is considered to have a favorable safety profile compared to natural LPS. By avoiding the complex heterogeneous mixture of LPS (which can contain toxic lipid A variants), RS-09 offers a more defined and potentially less toxic alternative. However, as a TLR4 agonist, high doses or systemic administration could potentially induce excessive inflammation, cytokine storm, or septic shock-like symptoms. Standard toxicological evaluation in animal models would monitor body weight, clinical signs, and cytokine levels.
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| References | |
| Additional Infomation |
RS-09 is a research-grade peptide and not a clinical drug. It represents a new class of peptide-based TLR4 agonists that serve as vaccine adjuvants. Compared to traditional adjuvants like alum or incomplete Freund's adjuvant (IFA), TLR4 agonists can induce a more balanced Th1/Th2 immune response. This compound allows researchers to investigate the mechanistic roles of TLR4 signaling in immune activation and to develop next-generation vaccine adjuvants. As of the latest updates, it has not been approved for clinical use and is exclusively available for research.
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| Molecular Formula |
C31H49N9O9
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|---|---|
| Molecular Weight |
691.775666952133
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| Exact Mass |
691.365
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| CAS # |
1449566-36-2
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| Related CAS # |
RS 09 TFA
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| PubChem CID |
155977542
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1191.2±65.0 °C at 760 mmHg
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| Flash Point |
674.2±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.586
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| LogP |
-1.89
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
63
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| Complexity |
1320
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@H](C(=O)N1CCC[C@H]1C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC3=CN=CN3)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)O)N.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O
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| InChi Key |
MKCNGKQUSQZTFM-AZNUZYABSA-N
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| InChi Code |
InChI=1S/C31H49N9O9.2C2HF3O2/c1-16(2)11-20(27(44)38-22(14-41)31(48)49)36-25(42)18(4)35-26(43)21(12-19-13-33-15-34-19)37-28(45)23-7-5-9-39(23)30(47)24-8-6-10-40(24)29(46)17(3)32;2*3-2(4,5)1(6)7/h13,15-18,20-24,41H,5-12,14,32H2,1-4H3,(H,33,34)(H,35,43)(H,36,42)(H,37,45)(H,38,44)(H,48,49);2*(H,6,7)/t17-,18-,20-,21-,22-,23-,24-;;/m0../s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoic acid;2,2,2-trifluoroacetic acid
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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) |
H2O : ~100 mg/mL (~144.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (144.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4455 mL | 7.2277 mL | 14.4555 mL | |
| 5 mM | 0.2891 mL | 1.4455 mL | 2.8911 mL | |
| 10 mM | 0.1446 mL | 0.7228 mL | 1.4455 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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