| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Interleukin-1beta (IL-1beta) and interleukin-1alpha (IL-1alpha). Goflikicept is a hybrid protein that selectively targets and neutralizes both circulating IL-1beta and IL-1alpha. By binding to these cytokines, it prevents their interaction with the IL-1 receptor (IL-1R1) and the co-receptor IL-1R accessory protein (IL-1RAcP), thereby blocking downstream NF-kappaB and MAPK signaling and reducing inflammation.
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| ln Vitro |
In vitro, Goflikicept binds to recombinant human IL-1beta and IL-1alpha with high affinity. It neutralizes the bioactivity of both cytokines in cell-based assays, blocking IL-1beta- and IL-1alpha-induced production of pro-inflammatory cytokines (e.g., IL-6, IL-8) and chemokines in human fibroblasts and endothelial cells. The IC50 for both IL-1beta and IL-1alpha is in the low nanomolar range.
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| ln Vivo |
In animal models of myocardial ischemia/reperfusion injury (such as the rat or mouse model of STEMI), Goflikicept reduces infarct size, preserves cardiac function, and decreases markers of systemic inflammation. Treatment with Goflikicept lowers serum levels of IL-6 and CRP and reduces neutrophil infiltration into damaged cardiac tissue, demonstrating its potential to mitigate the inflammatory response following acute MI.
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| Enzyme Assay |
A direct binding ELISA is performed to characterize antigen binding: recombinant human IL-1beta or IL-1alpha protein is immobilized on a microplate. Serially diluted Goflikicept is added, and bound fusion protein is detected using an HRP-conjugated anti-human Fc secondary antibody. The binding EC50 for each cytokine is calculated from the dose-response curve.
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| Cell Assay |
To measure functional neutralization, the IL-1beta-responsive MRC-5 human fibroblast cell line is used. MRC-5 cells are seeded into 96-well plates and stimulated with recombinant human IL-1beta (e.g., 0.1-1 ng/mL) or IL-1alpha (e.g., 0.1-1 ng/mL) in the presence of serially diluted Goflikicept (e.g., 0.01-100 ug/mL) for 24-48 hours. Supernatants are collected, and IL-6 or IL-8 levels are measured by ELISA. The IC50 for IL-1beta and IL-1alpha neutralization is calculated from the dose-response curve.
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| Animal Protocol |
The in vivo efficacy is evaluated in a rat model of myocardial ischemia/reperfusion injury (MI/R injury). Male Sprague-Dawley rats undergo left anterior descending (LAD) coronary artery ligation for 30-45 minutes (ischemia) followed by 2-24 hours of reperfusion. Goflikicept is administered intravenously (e.g., 1-10 mg/kg) immediately before reperfusion or intraperitoneally (e.g., 5-30 mg/kg) prior to ischemia. After the reperfusion period, the heart is excised for assessment of infarct size by triphenyltetrazolium chloride (TTC) staining and for measurement of cardiac function markers (e.g., troponin I). Blood samples are collected for measurement of serum IL-6, TNF-alpha, and CRP levels by ELISA.
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| ADME/Pharmacokinetics |
Goflikicept is a hybrid fusion protein with a molecular weight and PK properties similar to other Fc-fusion proteins. In rodents, the half-life is approximately 2-5 days. Cmax is dose-proportional after intravenous or intraperitoneal administration, and clearance is low. Bioavailability after subcutaneous injection is moderate (~50-70%).
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies indicate that Goflikicept is well-tolerated. No significant dose-limiting toxicities or major organ toxicities have been reported at therapeutic dose levels in animal models. As an IL-1 blocker, it may be associated with an increased risk of infections; however, such effects were not dose-limiting in research studies.
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| References | |
| Additional Infomation |
Goflikicept is currently in preclinical research phases and has not been investigated in clinical trials or approved for therapeutic use. It is a research-grade reagent available for laboratory studies investigating the role of IL-1alpha and IL-1beta in inflammatory diseases, particularly in the context of acute myocardial infarction and cardiovascular inflammation.
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| CAS # |
2416984-26-2
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| Appearance |
Colorless to light yellow liquid
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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 |
| 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) |
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
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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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