| Size | Price | Stock | Qty |
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| 100g |
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| Other Sizes |
| Targets |
The "target" of Wheat Gluten is the human immune system in genetically susceptible individuals (HLA-DQ2/DQ8). Gluten is not a drug; its biological activity is immunogenic. Specific proline-rich peptides derived from gliadin (e.g., 33-mer and 26-mer) resist complete digestion by gastric enzymes. These peptides are deamidated by tissue transglutaminase (TG2) in the intestinal mucosa. These deamidated peptides bind with high affinity to the HLA-DQ2/DQ8 molecules on antigen-presenting cells, which then activate CD4+ T-cells. This triggers an inflammatory cascade leading to villous atrophy and crypt hyperplasia, the hallmark of celiac disease.
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| ln Vitro |
In vitro activity of Wheat Gluten is measured by its ability to stimulate T-cells. Peripheral blood mononuclear cells (PBMCs) or intestinal T-cell lines derived from celiac disease patients are cultured in 96-well plates. They are stimulated with proteolytically digested gluten (pepsin/trypsin digest) or synthetic immunogenic peptides (e.g., the 33-mer deamidated gliadin peptide). The cell culture supernatant is harvested after 48-72 hours, and the concentration of pro-inflammatory cytokines (e.g., Interferon-gamma, IL-2, IL-15) is measured by ELISA. The extent of cytokine production is a direct measure of the in vitro activity of the gluten proteins. This assay is the gold standard for diagnosing celiac disease via "gluten challenge" experiments.
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| ln Vivo |
In vivo activity is the core pathology of celiac disease. When a sensitive individual ingests gluten, the immune reaction occurs in the small intestine. This leads to flattening of the villi (villus atrophy) and loss of the intestinal barrier. Symptoms include diarrhea, malabsorption, weight loss, and nutrient deficiencies. In research, gluten is used to induce this pathology in animal models (e.g., transgenic mice). The in vivo activity of gluten is the direct cause of the clinical symptoms. The amount of gluten ingested correlates with the degree of intestinal damage, as measured by Marsh score from duodenal biopsies. This specific in vivo effect has been well characterized and is the reason for the success of the gluten-free diet (GFD).
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| Enzyme Assay |
Non-cellular assays for Wheat Gluten are typically analytical methods to quantify its presence. A standard protocol uses a competitive ELISA with a gluten-specific monoclonal antibody (e.g., R5 or G12 antibody). The sample (e.g., food extract) is added to wells coated with an gliadin protein. A biotinylated detection antibody is added. After washing, streptavidin-HRP and substrate are added, and the absorbance is measured at 450 nm. The concentration of gluten is determined by comparing the absorbance to a standard curve of known gliadin concentrations. This assay is critical for validating the safety of "gluten-free" products. The limits of detection are typically <5 ppm.
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| Cell Assay |
Cellular assays to study gluten toxicity are often performed on intestinal biopsies or T-cell lines. A standard protocol uses human intestinal epithelial cell lines (e.g., Caco-2). Cells are grown to confluence on Transwell inserts to form a polarized monolayer. The apical side of the monolayer is treated with a digested gluten fraction (e.g., the "gliadin peptide"). Intestinal permeability is measured over time by adding a fluorescent marker (e.g., fluorescein isothiocyanate-dextran, FD-4) to the apical chamber and measuring its appearance in the basolateral chamber after 2-4 hours. An increase in FD-4 flux indicates that the gluten peptides disrupt the epithelial barrier (zonulin-mediated), mimicking the "leaky gut" seen in celiac patients.
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| Animal Protocol |
In vivo animal models for celiac disease typically use NOD/DQ8 transgenic mice. These mice are sensitized to gluten by intraperitoneal injection of gluten with an adjuvant. After sensitization, the mice are orally challenged with a gluten-containing diet for 3-4 weeks. The mice are then sacrificed, and the small intestine is removed for histology. Cross-sections of the duodenum are stained with hematoxylin and eosin (H&E). Key endpoints include the villus-to-crypt ratio (V/C ratio) and the number of intraepithelial lymphocytes (IELs) per 100 enterocytes. A decrease in V/C ratio and an increase in IEL count (a Marsh score of 1 or higher) confirms the development of an enteropathy, successfully modeling the disease.
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| ADME/Pharmacokinetics |
Wheat Gluten is a food ingredient, not a drug; hence, traditional pharmacokinetics is not relevant. However, the absorption of gluten peptides is studied. Immunogenic peptides (like the 33-mer) are relatively resistant to proteases and can be detected in human serum and urine after ingestion. The major route of elimination is fecal excretion. The half-life of the immunogenic peptides in circulation is short (minutes to hours), but the inflammatory response they trigger can last for weeks. The physiochemical property of gluten is its cohesive, visco-elastic proteinaceous nature, which enhances dough strength and mixing tolerance. It is used as a protein supplement in low-protein bread flours. It is a pale yellow powder, insoluble in water but soluble in weak acids and bases. It is stable if stored in a cool, dry place.
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| Toxicity/Toxicokinetics |
The toxicity of Wheat Gluten is dependent on the individual. For the general population, it is a nutritious protein. For people with celiac disease (1% of the population), it is a potent toxin that triggers an autoimmune response. Ingestion leads to intestinal damage, which increases the risk of gastrointestinal malignancies (e.g., lymphoma) if untreated. For people with wheat allergies, it can trigger anaphylaxis. The "Acute toxicity" (LD50) of gluten is not applicable as it is not acutely poisonous. Standard laboratory handling of the powder does not pose a direct chemical hazard, but it is a potential allergen and a respiratory sensitizer. When handled in bulk, dust masks should be worn to avoid inhalation, which can cause "baker's asthma." It is classified as a skin and eye irritant.
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| References | |
| Additional Infomation |
Wheat Gluten is not a drug but is one of the most important antigens in food science and medicine. The discovery of celiac disease's link to gluten was a landmark in medical history, leading to the development of the life-saving gluten-free diet (GFD). The only treatment for celiac disease is lifelong abstinence from gluten. In research, purified Wheat Gluten is an essential standard for developing diagnostic tests (ELISA for gluten in food) and for drug discovery (testing oral enzyme therapies that degrade gluten before it reaches the small intestine). Clinical trials are ongoing for agents like TAK-062 (a glutenase). Despite being a common food component, its profound biological effects in susceptible individuals make it a critical target for pharmaceutical intervention.
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| Molecular Formula |
C7H14CLNO2
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|---|---|
| Molecular Weight |
179.644561290741
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| CAS # |
8002-80-0
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| Appearance |
White to off-white solid powder
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| SMILES |
Cl.O(CC)C(C1CNCC1)=O
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| Synonyms |
Gluten Source Wheat
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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: Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5667 mL | 27.8334 mL | 55.6669 mL | |
| 5 mM | 1.1133 mL | 5.5667 mL | 11.1334 mL | |
| 10 mM | 0.5567 mL | 2.7833 mL | 5.5667 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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