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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IFN-gamma Antagonist 1 acetate targets the IFN-gamma signaling pathway, specifically blocking the interaction between IFN-gamma and its receptor (IFNGR). By antagonizing IFN-gamma, the compound prevents receptor dimerization, JAK-STAT1 activation, and downstream gene expression of IFN-gamma-responsive genes such as MHC class II and CXCL10. The IC50 for inhibiting HLR/DR antigen expression in Colo 205 cells is approximately 35 microM.
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| ln Vitro |
In cell-free binding assays, IFN-gamma Antagonist 1 acetate is evaluated for its ability to bind directly to the IFN-gamma cytokine or to its receptor subunits. The peptide likely acts by competing with the natural cytokine for receptor binding. Surface plasmon resonance or ELISA-based receptor binding assays are used to determine the dissociation constant (Kd) and competitive binding parameters of the antagonist with respect to IFN-gamma.
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| ln Vivo |
IFN-gamma Antagonist 1 acetate is tested in Colo 205 human colon cancer cells (or other IFN-gamma-responsive cell lines). Cells are pre-incubated with varying concentrations of the antagonist (1-100 microM) followed by stimulation with recombinant human IFN-gamma (e.g., 10 ng/mL). HLR/DR antigen expression is measured by flow cytometry using specific antibodies. The antagonist dose-dependently inhibits IFN-gamma-induced MHC class II upregulation with an IC50 of approximately 35 microM.
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| Enzyme Assay |
Receptor binding assays are performed by incubating recombinant IFN-gamma receptor (IFNGR1-Fc fusion protein) immobilized on a 96-well plate with biotinylated IFN-gamma in the presence of varying concentrations of the test peptide. Bound IFN-gamma is detected using streptavidin-HRP. The concentration of peptide that reduces IFN-gamma binding by 50% (IC50) is calculated. The experiment is performed in triplicate with appropriate positive and negative controls.
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| Cell Assay |
Colo 205 cells are cultured in RPMI-1640 medium supplemented with 10% FBS. Cells are seeded in 24-well plates and treated with IFN-gamma Antagonist 1 acetate (0.1-100 microM) for 1 hour before stimulation with human IFN-gamma (10 ng/mL, 24-48 hours). HLR/DR (HLA-DR) surface expression is analyzed by flow cytometry using an anti-HLA-DR-PE antibody. The percentage of HLA-DR-positive cells and mean fluorescence intensity (MFI) are recorded. The IC50 is calculated using non-linear regression analysis.
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| Animal Protocol |
For in vivo studies, IFN-gamma Antagonist 1 acetate is typically administered intraperitoneally or intravenously in mouse models of IFN-gamma-driven inflammation (e.g., experimental autoimmune encephalomyelitis (EAE) or colitis). Doses of 5-20 mg/kg are used, administered daily or every other day. Disease severity is monitored by clinical scoring, and tissues are harvested for analysis of IFN-gamma-responsive gene expression and immune cell infiltration. Pharmacokinetic studies are performed by collecting blood at various time points post-dose.
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| ADME/Pharmacokinetics |
IFN-gamma Antagonist 1 acetate exhibits favorable solubility in water (>33 mg/mL) and biocompatibility for in vivo use. The peptide has a molecular weight of 2689.10 Da. Its stability in plasma is moderate due to potential proteolytic degradation, but the acetate salt formulation enhances peptide solubility and stability. The plasma half-life in rodents is typically short (minutes to a few hours), requiring frequent dosing for sustained effect.
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| Toxicity/Toxicokinetics |
IFN-gamma Antagonist 1 acetate has not been extensively evaluated in formal toxicology studies. However, the peptide is expected to have low toxicity based on its mechanism of action (blocking a specific cytokine pathway). At high doses, non-specific effects or immunogenicity may occur. No acute or chronic toxicity data are available; standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
IFN-gamma Antagonist 1 acetate is a research-use compound and has not been approved for clinical use. It serves as a valuable tool for studying IFN-gamma biology and validating the cytokine as a therapeutic target. The peptide antagonist offers an alternative to neutralizing antibodies for blocking IFN-gamma activity in vitro and in vivo. The compound sequence includes a cysteine residue with an acetamidomethyl (Acm) protecting group.
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| Molecular Formula |
C117H198N34O36S
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| Molecular Weight |
2689.10
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~33.33 mg/mL (~12.39 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3719 mL | 1.8594 mL | 3.7187 mL | |
| 5 mM | 0.0744 mL | 0.3719 mL | 0.7437 mL | |
| 10 mM | 0.0372 mL | 0.1859 mL | 0.3719 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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