| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
alpha-Casein (90-95) TFA targets opioid receptors, acting as a partial agonist. It also functions as a copper ion ligand. The peptide has been shown to inhibit beta-hexosaminidase secretion from rat peritoneal mast cells (IC50 = 0.1 microM), suggesting activity at mast cell receptors. It activates Gi-like proteins through a membrane-assisted, receptor-independent pathway or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes. The peptide also inhibits the proliferation of prostate cancer cells (LNCaP, DU145, PC3).
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| ln Vitro |
In vitro, alpha-Casein (90-95) TFA is a partial agonist of opioid receptors. It inhibits the secretion of beta-hexosaminidase from rat peritoneal mast cells (PMC) with an IC50 of 0.1 microM. It also inhibits the proliferation of prostate cancer cells, with IC50 values of 0.94 nM (LNCaP), 137 nM (DU145), and 6.92 nM (PC3). The peptide activates Gi-like proteins and induces intracellular calcium release. It exhibits opioid activity and can be used to study the mechanisms of allergic diseases and prostate cancer.
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| ln Vivo |
In vivo activity data for alpha-Casein (90-95) TFA are not extensively published. As a partial opioid receptor agonist, it is hypothesized to have potential effects on pain perception, gastrointestinal motility, and immune function. The peptide's ability to inhibit mast cell degranulation suggests potential anti-allergic effects in animal models. Further in vivo studies are required to validate its systemic efficacy and pharmacokinetics.
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| Enzyme Assay |
For in vitro receptor binding assays, membranes prepared from cells expressing opioid receptor subtypes (micro, delta, kappa) are incubated with a radiolabeled opioid ligand (e.g., [3H]-DAMGO for micro receptors, [3H]-DPDPE for delta receptors, or [3H]-U-69593 for kappa receptors) in the presence of increasing concentrations of alpha-Casein (90-95) TFA (0.001-100 uM). Non-specific binding is determined using 10 uM naloxone. After incubation at room temperature for 60 minutes, bound radioligand is separated by filtration, and radioactivity is counted. Ki values are calculated from competition curves.
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| Cell Assay |
For mast cell degranulation assays, rat peritoneal mast cells (PMCs) are isolated and pre-incubated with alpha-Casein (90-95) TFA at various concentrations (0.01-100 uM) for 15-30 minutes at 37degC. Cells are then stimulated with a degranulation inducer (e.g., compound 48/80 or A23187). After 30 minutes, the reaction is stopped by centrifugation. The supernatant is collected to measure beta-hexosaminidase activity using a chromogenic substrate (p-nitrophenyl-N-acetyl-beta-D-glucosaminide) at 405 nm. The percentage of inhibition of degranulation is calculated, and the IC50 is determined. For prostate cancer cell proliferation assays, LNCaP, DU145, and PC3 cells are seeded in 96-well plates. After 24 hours, cells are treated with alpha-Casein (90-95) TFA at concentrations ranging from 0.01 nM to 100 uM. After 48-72 hours, cell viability is assessed using MTT or CellTiter-Glo assays. The IC50 is calculated using dose-response curve fitting. Apoptosis can be measured by flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
In vivo protocols for alpha-Casein (90-95) TFA are not well-documented in the public literature. To study potential anti-allergic effects, a passive cutaneous anaphylaxis (PCA) model in rats could be used. The peptide would be administered intravenously or intraperitoneally at doses ranging from 0.1-10 mg/kg, followed by an antigen challenge. Mast cell degranulation in the skin would be measured by Evans blue dye extravasation. For pain studies, a tail-flick or hot plate test could be used after intrathecal administration.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for alpha-Casein (90-95) TFA are not available. As a hexapeptide with a molecular weight of 897.94 Da, it is unlikely to be orally bioavailable. It is expected to have a short half-life in plasma due to rapid proteolytic degradation. For in vitro studies, the peptide is soluble in water and DMSO. Stock solutions can be stored at -20degC or -80degC. The lyophilized powder should be stored at -20degC, protected from moisture.
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| Toxicity/Toxicokinetics |
Toxicological data for alpha-Casein (90-95) TFA are limited. In cell-based assays at concentrations up to 10 uM, no significant cytotoxicity is reported. The peptide's opioid activity suggests potential for central nervous system effects (analgesia, sedation, respiratory depression) at high doses. Comprehensive toxicology studies have not been published. Standard safety precautions for handling peptides should be followed.
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| Additional Infomation |
alpha-Casein (90-95) TFA is a research-grade peptide and is not approved for clinical use. Its hexapeptide sequence is Arg-Tyr-Leu-Gly-Tyr-Leu (RYLGYL). The molecular weight is 897.94, and the molecular formula is C40H58F3N9O11. The peptide is a partial agonist of opioid receptors and a copper ion ligand. It is used as a tool to study opioid signaling, mast cell function, allergic diseases, and prostate cancer mechanisms. Store at -20degC as a lyophilized powder, protected from light and moisture.
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| Molecular Formula |
C40H58F3N9O11
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| Molecular Weight |
897.94
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| Related CAS # |
α-Casein (90-95);83471-50-5
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| Appearance |
Typically exists as solid at room temperature
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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) |
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 | 1.1137 mL | 5.5683 mL | 11.1366 mL | |
| 5 mM | 0.2227 mL | 1.1137 mL | 2.2273 mL | |
| 10 mM | 0.1114 mL | 0.5568 mL | 1.1137 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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