| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Peptide 401 is the mast cell. It acts as a potent mast cell degranulating factor by binding to the cell surface and triggering the release of histamine from peritoneal mast cells. This degranulation is a key event in allergic and inflammatory responses. While the exact receptor is not fully defined, it is known to induce a rapid release of histamine and other vasoactive mediators. It also suppresses the increased vascular permeability caused by various smooth muscle spasmogens like histamine and 5-HT.
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| ln Vitro |
In vitro, Peptide 401 is a potent inducer of mast cell degranulation. It activates histamine release from peritoneal mast cells. It also exhibits anti-inflammatory activity, as it can suppress the increased vascular permeability induced by various smooth muscle spasmogens such as histamine and 5-HT. It is used in a wide range of studies, from enzymology to receptor binding assays and cell signaling research, to understand mast cell biology and inflammation.
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| ln Vivo |
When rats were injected with turpentine into the joint or carrageenan into the plantar foot, peptide 401 dramatically reduced the amount of swelling that resulted. 401 has an ED50 of c. 0.1 mg/kg. By comparing the injected site's elevated 125I-albumin level to the contralateral site that was left uninjected, the anti-inflammatory impact was evaluated. Additionally, Peptide 401 prevents the rise in vascular permeability brought on by intradermal injections of prostaglandins, histamine, bradykinin, serotonin (5-HT), and other smooth muscle spasmodics [1]. The common European honey bee's venom contains 22 residues of peptide 401, often known as the MCD peptide, which makes up around 2% of the total weight. In several animal models, including rats with adjuvant arthritis, carrageenan- or turpentine-induced hindpaw edema, and increased skin permeability, it demonstrates strong anti-inflammatory activity (at doses as low as 0.1 mg/kg). Subcutaneous injections of bradykinin, prostaglandin E1, kallikrein, histamine, and 5-hydroxytryptamine (5-HT) were given to sexual rats. Histamine and other pharmacologically active substances are released, and it has strong degranulation effects on mast cells [2].
In vivo, Peptide 401 has been shown to have anti-inflammatory activity. In animal models, it decreases paw edema. It has demonstrated anti-inflammatory activity in a mouse model of carrageenan-induced inflammation. These effects are paradoxical, as it both induces mast cell degranulation (a pro-inflammatory event) and suppresses inflammation. This dual activity makes it a unique tool for studying the complex role of mast cells in the inflammatory response. |
| Enzyme Assay |
Cell-free receptor binding assays for Peptide 401 are not typical, as its primary target is the mast cell, a whole cell. However, its binding to components of the mast cell membrane can be studied. A protocol involves isolating mast cell membranes and incubating them with a radiolabeled Peptide 401 (e.g., [125I]-Peptide 401) and varying concentrations of unlabeled peptide. Bound and free ligand are separated by centrifugation, and the radioactivity is measured. This allows for the characterization of its binding affinity to the mast cell surface.
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| Cell Assay |
For in vitro cellular experiments, peritoneal mast cells are isolated from rodents and cultured in appropriate media. Cells are treated with Peptide 401 at various concentrations (typically 0.1-100 ug/mL) for a short period (e.g., 15-30 minutes). Mast cell degranulation is assessed by measuring the release of histamine or beta-hexosaminidase into the supernatant using ELISA or fluorometric assays. The compound's potency (EC50) and efficacy are determined from the dose-response curve.
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| Animal Protocol |
In vivo animal experiments with Peptide 401 are conducted to study its anti-inflammatory effects. A common protocol involves inducing paw edema in mice by injecting carrageenan into the paw. Peptide 401 is administered at various doses (e.g., 0.1-10 mg/kg) via intraperitoneal (IP) injection, either prophylactically or therapeutically. The anti-inflammatory effect is assessed by measuring the reduction in paw swelling over time using a plethysmometer. The reduction in paw edema indicates the compound's anti-inflammatory activity.
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| ADME/Pharmacokinetics |
Peptide 401 is a peptide with a molecular weight of 2587.22 g/mol and a molecular formula of C110H192N40O24S4. It is a 22-amino acid peptide with two disulfide bridges. As a peptide, it is typically administered by injection in experimental settings. Its half-life in vivo is short due to proteolytic degradation. It is stable as a powder and should be stored at -20degC. It is soluble in aqueous buffers. Its pharmacokinetic properties are consistent with those of a peptide, characterized by rapid clearance.
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| Toxicity/Toxicokinetics |
The toxicity profile of Peptide 401 is related to its potent mast cell degranulating activity. It can cause a massive release of histamine and other inflammatory mediators, leading to anaphylactic shock if administered systemically at high doses. However, at lower doses, it has been shown to have anti-inflammatory effects. The compound is for research use only and not for human therapeutic use. Due to its potency, it should be handled with extreme care in a controlled laboratory environment.
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| References |
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| Additional Infomation |
Peptide 401, also known as the mast cell degranulating (MCD) peptide, is a 22-amino acid peptide isolated from bee venom. It is a potent inducer of mast cell degranulation, causing the release of histamine. Paradoxically, it also exhibits anti-inflammatory activity, reducing paw edema in animal models. It is a valuable research tool for studying mast cell biology, inflammation, and the development of anti-inflammatory agents. It is not approved for clinical use.
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| Molecular Formula |
C110H192N40O24S4
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|---|---|
| Molecular Weight |
2587.21508
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| Exact Mass |
2585.39
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| CAS # |
32908-73-9
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| PubChem CID |
16132290
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| Appearance |
White to off-white solid powder
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| LogP |
6.11
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| Hydrogen Bond Donor Count |
35
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| Hydrogen Bond Acceptor Count |
38
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| Rotatable Bond Count |
58
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| Heavy Atom Count |
178
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| Complexity |
5670
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| Defined Atom Stereocenter Count |
0
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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, 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 | 0.3865 mL | 1.9326 mL | 3.8652 mL | |
| 5 mM | 0.0773 mL | 0.3865 mL | 0.7730 mL | |
| 10 mM | 0.0387 mL | 0.1933 mL | 0.3865 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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