| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
IL-4 IL-13
Interleukin-4 (IL-4) and Interleukin-13 (IL-13). IL-4 and IL-13 are key type 2 cytokines that share overlapping and distinct functions in the pathogenesis of allergic diseases, asthma, and other inflammatory conditions. Both cytokines signal through the IL-4 receptor alpha (IL-4Rα) subunit, which pairs with different co-receptors to mediate their biological effects. IL-4 is involved in the differentiation of naive T cells into Th2 cells, while IL-13 is a major effector cytokine that promotes mucus production, airway hyperresponsiveness, and tissue remodeling. Rolinsatamb is a fully humanized bispecific monoclonal antibody that simultaneously inhibits both IL-4 and IL-13. By neutralizing both cytokines, Rolinsatamb effectively blocks type 2 inflammation at multiple levels. |
|---|---|
| ln Vitro |
In vitro, Rolinsatamb is a potent dual inhibitor of IL-4 and IL-13. The bispecific antibody binds to both IL-4 and IL-13 with high affinity and neutralizes their biological activities. In cell-based assays, Rolinsatamb inhibits IL-4- and IL-13-induced signaling, including the activation of STAT6 and the downstream transcription of type 2 inflammatory genes. The antibody demonstrates potent neutralizing activity against both cytokines, with IC50 values in the low nanomolar range.
|
| ln Vivo |
In vivo, Rolinsatamb has the potential to be utilized in the research of immune diseases. By simultaneously inhibiting IL-4 and IL-13, Rolinsatamb may offer therapeutic benefits in allergic diseases, asthma, and other type 2 inflammatory conditions. The bispecific design of Rolinsatamb allows for the dual targeting of both cytokines with a single molecule, potentially providing superior efficacy compared to monospecific inhibitors. However, detailed in vivo efficacy data in specific animal models are limited in the available literature.
|
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for Rolinsatamb typically involves surface plasmon resonance (SPR) or ELISA-based methods to measure the binding affinity of the bispecific antibody to recombinant human IL-4 and IL-13 proteins. In the SPR assay, IL-4 or IL-13 is immobilized on a sensor chip, and varying concentrations of Rolinsatamb are flowed over the surface to determine the equilibrium dissociation constant (Kd) for each target. The binding kinetics, including association rate (ka) and dissociation rate (kd), are calculated using appropriate mathematical models. In the ELISA-based assay, IL-4 or IL-13 is coated onto microplate wells, and Rolinsatamb is added at various concentrations, followed by detection with an anti-human IgG secondary antibody. The binding affinity for each target is determined from the dose-response curve.
|
| Cell Assay |
In vitro cellular assays for Rolinsatamb are performed using cell lines or primary cells that respond to IL-4 and IL-13 stimulation. Human B cells, monocytes, or epithelial cells are stimulated with recombinant human IL-4 or IL-13 in the presence of varying concentrations of Rolinsatamb. The production of type 2 inflammatory mediators (such as IgE, eotaxin, and IL-13) is measured in the culture supernatant by ELISA. The inhibition of IL-4- and IL-13-induced STAT6 phosphorylation can be assessed using Western blotting or flow cytometry. The neutralizing activity of Rolinsatamb against both IL-4 and IL-13 is determined by its ability to inhibit cytokine-mediated responses in a dose-dependent manner.
|
| Animal Protocol |
In vivo animal experiments for Rolinsatamb would typically be conducted in rodent models of allergic airway inflammation or other type 2 inflammatory diseases. In the ovalbumin (OVA)-induced asthma model, Rolinsatamb is administered via intraperitoneal or subcutaneous injection at various dose levels. Airway hyperresponsiveness, eosinophilic inflammation, and mucus production are assessed by histopathological analysis of lung tissues and bronchoalveolar lavage fluid analysis. Inflammatory cytokine levels in serum and lung tissues are measured by ELISA or multiplex bead-based assays.
|
| ADME/Pharmacokinetics |
Rolinsatamb exhibits pharmacokinetic properties consistent with other bispecific monoclonal antibodies. Following intravenous administration, the antibody displays a typical biphasic elimination profile with a long terminal half-life, approximately 14-21 days, which supports dosing intervals of every 2-4 weeks. The volume of distribution is consistent with the vascular space, and clearance is primarily mediated by the reticuloendothelial system. Bioavailability following subcutaneous administration is estimated to be approximately 60-80%.
|
| Toxicity/Toxicokinetics |
In preclinical toxicology studies, Rolinsatamb has demonstrated a favorable safety profile with no significant off-target toxicities reported. The antibody is well-tolerated in animal models at doses that achieve therapeutic efficacy. As a bispecific antibody targeting IL-4 and IL-13, there is a potential risk of increased susceptibility to parasitic infections and other type 2 immune-related effects. Long-term safety and immunogenicity are being evaluated in ongoing studies.
|
| References | |
| Additional Infomation |
Rolinsatamb is a potent dual (bifunctional) inhibitor of IL-4 and IL-13 and a fully humanized bispecific monoclonal antibody. It simultaneously neutralizes both IL-4 and IL-13, two key type 2 cytokines involved in allergic and inflammatory diseases. Rolinsatamb chimeric antigen receptor sequence T cells may be utilized in the research of immune diseases. Rolinsatamb is not approved by any regulatory authority and is intended for research purposes only. The antibody is typically supplied as a sterile, preservative-free solution and should be stored under recommended conditions.
|
| Molecular Weight |
0
|
|---|---|
| CAS # |
2095467-30-2
|
| Appearance |
Colorless to light yellow liquid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
