IL 1RA Human

Interleukin-1 Receptor Antagonist Human Recombinant
Cat. No.
BT944
Source
Escherichia Coli.
Synonyms
IRAP, IL1F3, IL1RA, IL-1ra3, ICIL-1RA, IL1RN, IL1 inhibitor, IL-1ra, MGC10430.
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by:
(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
Usage
THE BioTek's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.
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Description

IL1ra Human Recombinant produced in E.Coli is a non-glycosylated, N-terminal methionyl form of the human naturally-occurring polypeptide chain containing 153 amino acids and having a molecular mass of 17000 Dalton.
The IL1ra is purified by proprietary chromatographic techniques.

Product Specs

Introduction
Interleukin-1 receptor antagonist (IL-1ra) is a cytokine belonging to the interleukin 1 family. It acts as an inhibitor of interleukin 1, specifically IL1A and IL1B, effectively modulating a wide array of immune and inflammatory responses associated with interleukin 1. The gene encoding IL-1ra, along with five other closely related cytokine genes, forms a gene cluster spanning approximately 400 kb on chromosome 2. Notably, a polymorphism in this gene has been linked to an elevated risk of osteoporosis-related fractures and gastric cancer. Furthermore, four alternatively spliced transcript variants, which encode distinct isoforms of IL-1ra, have been identified.
Description
Recombinant human IL1ra produced in E. coli is a non-glycosylated protein. This specific form is a methionyl version of the naturally occurring human polypeptide chain. It consists of 153 amino acids, has a molecular weight of 17 kDa, and lacks glycosylation modifications. The purification process of IL1ra involves proprietary chromatographic methods.
Physical Appearance
White powder that has been sterilized through filtration and lyophilized.
Formulation
The protein is provided in a lyophilized form without any additional additives.
Solubility
To reconstitute the lyophilized Interleukin-1 ra, it is recommended to dissolve it in sterile 18M-cm H2O at a concentration of at least 100 µg/ml. This solution can be further diluted in other aqueous solutions as needed.
Stability
Lyophilized Interleukin 1ra demonstrates stability at room temperature for a period of 3 weeks. However, for extended storage, it is recommended to store it in a desiccated state at a temperature below -18°C. After reconstitution, IL-1ra should be stored at 4°C for a duration of 2-7 days. For long-term storage, it is advisable to store it below -18°C. To ensure optimal stability during long-term storage, the addition of a carrier protein (0.1% HSA or BSA) is recommended. It is important to minimize freeze-thaw cycles.
Purity
The purity of the protein is greater than 98.0%, as determined by the following methods: (a) Reverse-phase high-performance liquid chromatography (RP-HPLC) analysis and (b) Sodium dodecyl-sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis.
Biological Activity
The ED50 value, representing the dose at which 50% inhibition is observed, was determined to be 0.5 ng/ml. This value was derived from an assay assessing the dose-dependent inhibition of IL-1-induced stimulation of D10S cells. This corresponds to a Specific Activity of 2,000,000 IU/mg.
Protein Content
Protein quantification was performed using two independent methods. The first method involved UV spectroscopy at a wavelength of 280 nm. An absorbency value of 0.89 was used as the extinction coefficient for a 0.1% (1 mg/ml) solution. This value was calculated using the PC GENE computer analysis program, which analyzes protein sequences (IntelliGenetics). The second method employed RP-HPLC analysis using a standard solution of IL-1ra as a reference standard.
Synonyms
IRAP, IL1F3, IL1RA, IL-1ra3, ICIL-1RA, IL1RN, IL1 inhibitor, IL-1ra, MGC10430.
Source
Escherichia Coli.
Amino Acid Sequence
The sequence of the first five N-terminal amino acids was determined and was found to be Met-Arg-Pro-Ser-Gly.

Product Science Overview

Introduction

Interleukin-1 Receptor Antagonist (IL-1Ra) is a naturally occurring protein that plays a crucial role in regulating the immune response by inhibiting the activities of interleukin-1 (IL-1). The recombinant form of this protein, known as Human Recombinant IL-1Ra, has been developed for therapeutic purposes, particularly in the treatment of inflammatory diseases such as rheumatoid arthritis.

Discovery and Development

IL-1Ra was first discovered in 1984 in the urine and serum of patients with leukemia and in the supernatant of cultured monocytes . The protein was named for its ability to competitively bind to the IL-1 receptor, thereby antagonizing the function of IL-1. This discovery paved the way for the development of recombinant forms of IL-1Ra for therapeutic use.

Recombinant Human IL-1Ra

Recombinant Human IL-1Ra (rHuIL-1Ra) is produced using recombinant DNA technology. One of the most well-known forms of rHuIL-1Ra is anakinra, marketed under the brand name Kineret™ . Anakinra differs from the native IL-1Ra by the addition of an N-terminal methionine, but it binds to the IL-1 receptor with the same affinity as IL-1β .

Mechanism of Action

IL-1Ra functions by binding to the IL-1 receptor type I (IL-1R1) without eliciting a signal, thereby blocking the binding and activity of IL-1α and IL-1β. This inhibition of IL-1 signaling helps to reduce inflammation and tissue damage associated with various inflammatory diseases .

Clinical Applications

Recombinant IL-1Ra has been extensively studied and used in the treatment of rheumatoid arthritis (RA). Clinical trials have demonstrated that anakinra, in combination with methotrexate (MTX), is effective in reducing the signs and symptoms of RA in patients who have inadequate responses to MTX alone . Anakinra has also been investigated for its potential use in other inflammatory conditions and diseases.

Pharmacokinetics and Safety

The pharmacokinetics and safety of recombinant IL-1Ra have been evaluated in various studies. For example, a study conducted on healthy Chinese subjects assessed the pharmacokinetics and safety of a recombinant human IL-1Ra candidate drug, GR007 . The results showed that a single intramuscular injection of GR007 had good safety and tolerability, with no serious adverse events reported .

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