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| 1mg |
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| Other Sizes |
| Targets |
Interferon-alpha (IFNα). Sifalimumab is an anti-IFNα monoclonal antibody that binds to multiple interferon-alpha subtypes. By binding to IFNα, the antibody suppresses the abnormal immune activity associated with elevated type I interferon signaling. IFNα is a key cytokine involved in the pathogenesis of systemic lupus erythematosus (SLE), and its neutralization reduces the interferon signature and downstream inflammatory responses.
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| ln Vitro |
Sifalimumab (3–36 μg/well; 72 h) reduces the cytotoxicity of lymphocytes co-cultured with U-87MG [2].
Sifalimumab binds to multiple interferon-alpha (IFNα) subtypes and suppresses abnormal immune activity. The antibody neutralizes IFNα, reducing the type I interferon signature that is elevated in SLE patients. By blocking IFNα signaling, Sifalimumab inhibits the downstream inflammatory responses and immune dysregulation associated with SLE. |
| ln Vivo |
Treatment with subcutaneous injection of sifelimumab (30 mg/kg and 3 μg/g) has a beneficial impact and reduces the infiltration of lymphocytes[2].
In vivo, Sifalimumab (subcutaneous injection; 30 mg/kg and 3 µg/g) shows therapeutic effect and attenuates lymphocyte infiltration. Clinical studies have evaluated Sifalimumab for the treatment of moderate-to-severe systemic lupus erythematosus (SLE). The antibody's ability to neutralize IFNα and reduce the interferon signature has demonstrated clinical benefit in SLE patients. Sifalimumab has been investigated in Phase 2b clinical trials for SLE. |
| Enzyme Assay |
Binding assays are used to measure the affinity of Sifalimumab for IFNα subtypes. Surface plasmon resonance or ELISA-based assays are performed with recombinant human IFNα subtypes, and increasing concentrations of Sifalimumab are added to determine binding affinity. The antibody's ability to bind multiple IFNα subtypes is assessed to confirm its broad neutralizing activity.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: U-87MG cells and AGS lymphocytes Tested Concentrations: 3-36 μg/well Incubation Duration: 72 hrs (hours) Experimental Results: Attenuated lymphocyte cytotoxicity triggered by IFN I (P<0.05). Cellular assays using IFNα-responsive cells are employed to evaluate the functional inhibition of Sifalimumab. Cells (e.g., peripheral blood mononuclear cells or IFNα-responsive reporter cell lines) are stimulated with IFNα in the presence of increasing concentrations of Sifalimumab. Inhibition of IFNα-induced signaling (e.g., STAT1 phosphorylation) and downstream gene expression is measured. The antibody's ability to suppress the interferon signature is assessed. |
| Animal Protocol |
Animal/Disease Models: Wild-type male BALB/c mice[2]
Doses: 30 mg/kg and 3 μg/g Route of Administration: subcutaneous (sc) injection; 30 mg/kg and 3 μg/g Experimental Results: Prevented the increase CpG-induced, decreasing CD86 fluorescence intensity by 1.9-fold (P < 0.05). demonstrated a potential therapeutic effect attenuating the CpG-induced lymphocyte infiltration. Attenuated the CD45 increase (P<0.05). In vivo efficacy of Sifalimumab has been evaluated in clinical trials in patients with moderate-to-severe systemic lupus erythematosus. The antibody is administered via subcutaneous or intravenous injection. Efficacy endpoints include reduction of disease activity (measured by SLEDAI or BILAG scores), reduction of the interferon signature, and improvement in quality of life. Phase 2b clinical trials have demonstrated clinical benefit in SLE patients. |
| ADME/Pharmacokinetics |
As a human IgG1 monoclonal antibody with molecular weight of 144.24 kDa, Sifalimumab is administered via parenteral routes (subcutaneous or intravenous). The IgG1 isotype provides Fc-mediated effector functions. Pharmacokinetic properties are characteristic of monoclonal antibodies with low immunogenicity. The antibody has been studied in clinical trials for SLE with a manageable safety profile.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated the safety of Sifalimumab in animal models. As an IFNα inhibitor, potential toxicities include increased susceptibility to viral infections, as IFNα plays a critical role in antiviral defense. Standard toxicology assessments include evaluation of immunogenicity and tissue cross-reactivity. Clinical trials have assessed the safety profile in SLE patients, with infections being a potential concern.
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| References |
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| Additional Infomation |
Sifalimumab (also known as MEDI-545 and MDX 1103) is an anti-IFNα monoclonal antibody. It is an immunoglobulin G1, anti-(human interferon α) human monoclonal antibody. Sifalimumab suppresses abnormal immune activity by binding to multiple IFNα subtypes. It has been developed for the treatment of moderate-to-severe systemic lupus erythematosus (SLE). Sifalimumab has been evaluated in Phase 2b clinical trials for SLE. CAS: 1006877-41-3.
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| CAS # |
1006877-41-3
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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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