| Size | Price | Stock | Qty |
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| Targets |
The IL-6 receptor binds to IL-6 with high affinity, and the IL-6/IL-6R complex subsequently associates with gp130 to form a hexameric signaling complex. This triggers activation of the JAK/STAT3, MAPK, and PI3K/Akt signaling pathways, leading to gene expression changes that regulate inflammation, cell proliferation, and differentiation.
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| ln Vitro |
In cell-free assays, purified IL-6 receptor demonstrates specific binding to IL-6 with a dissociation constant (Kd) in the nanomolar range. The interaction can be competitively inhibited by IL-6R antibodies or small-molecule inhibitors, as measured by surface plasmon resonance or ELISA-based binding assays.
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| ln Vivo |
In cell-based models, IL-6R inhibitors block IL-6-induced proliferation of B9 hybridoma or TF-1 cells. For example, tocilizumab (a humanized anti-IL-6R antibody) effectively inhibits IL-6-mediated signaling in multiple myeloma and rheumatoid arthritis synovial fibroblast cell lines, reducing STAT3 phosphorylation and downstream gene expression.
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| Enzyme Assay |
The binding affinity between IL-6 and its receptor is assessed using a cell-free ELISA where recombinant IL-6R is immobilized on a plate, and biotinylated IL-6 is added. Bound IL-6 is detected with streptavidin-HRP. Alternatively, surface plasmon resonance is used to determine kinetic parameters (ka, kd) and the dissociation constant (Kd).
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| Cell Assay |
For cellular assays, cells expressing IL-6R (e.g., U266 multiple myeloma cells or Ba/F3-gp130 cells) are serum-starved and stimulated with IL-6 in the presence or absence of test compounds. IL-6R activation is measured by STAT3 phosphorylation using phospho-specific antibodies in Western blot or flow cytometry. Proliferation is assessed by MTT or [3H]-thymidine incorporation.
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| Animal Protocol |
In animal models, IL-6R inhibitors are evaluated in collagen-induced arthritis (CIA) mice or IL-6 transgenic mice. For instance, anti-IL-6R antibodies are administered intraperitoneally (5-10 mg/kg, twice weekly) starting from arthritis onset. Disease severity is assessed by clinical scoring, paw swelling measurement, and histopathological analysis of joint sections.
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| ADME/Pharmacokinetics |
Monoclonal antibodies targeting IL-6R (e.g., tocilizumab, sarilumab) exhibit typical antibody-like pharmacokinetics: slow clearance, long half-life (7-14 days in humans), and subcutaneous/intravenous bioavailability. Small-molecule IL-6R inhibitors, if developed, may show different PK profiles depending on their chemical properties. Tissue distribution is primarily within the vascular and lymphatic compartments.
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| Toxicity/Toxicokinetics |
Clinically approved IL-6R inhibitors such as tocilizumab and sarilumab have well-characterized safety profiles. Common adverse events include upper respiratory tract infections, headache, and injection site reactions. Rare but serious risks include gastrointestinal perforation and hepatotoxicity. Long-term safety monitoring is recommended for patients on chronic therapy.
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| Additional Infomation |
Several IL-6R inhibitors have been approved for clinical use, including tocilizumab (Actemra®) for rheumatoid arthritis, juvenile idiopathic arthritis, and cytokine release syndrome; sarilumab (Kevzara®) for rheumatoid arthritis; and vobarilizumab (ALX-0061) in development. Ongoing research explores IL-6R inhibition for idiopathic pulmonary fibrosis, Parkinson‘s disease, and type 2 diabetes.
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| Molecular Formula |
C51H85N13O21
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|---|---|
| Molecular Weight |
1216.30
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| Sequence |
Thr-Ser-Leu-Pro-Val-Gln-Asp-Ser-Ser-Ser-Val-ProTSLPVQDSSSVP
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| SequenceShortening |
TSLPVQDSSSVP
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| Appearance |
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) |
H2O :~50 mg/mL (~41.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (41.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), Clear solution.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8222 mL | 4.1108 mL | 8.2217 mL | |
| 5 mM | 0.1644 mL | 0.8222 mL | 1.6443 mL | |
| 10 mM | 0.0822 mL | 0.4111 mL | 0.8222 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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