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αs1-CN f(143–149) acetate

αs1-CN f(143–149) acetate is an orally effective casein-derived peptide sequence.
αs1-CN f(143–149) acetate
αs1-CN f(143–149) acetate Chemical Structure Product category: ACE
This product is for research use only, not for human use. We do not sell to patients.
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1mg
5mg
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Other Forms of αs1-CN f(143–149) acetate:

  • αs1-CN f(143–149)
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Top Publications Citing lnvivochem Products
Product Description
αs1-CN f(143–149) acetate is an orally active casein-derived peptide sequence. αs1-CN f(143–149) acetate exhibits angiotensin-converting enzyme (ACE) inhibitory activity (IC50 = 6.58 μM) and antihypertensive activity.
alphas1-CN f(143-149) acetate (alphas1-casein fragment 143-149) is a bioactive peptide with the sequence Gly-Lys-Leu-Lys-Lys-Ile-Asn (GKLKKIN). It is derived from bovine alphas1-casein, a milk protein. This heptapeptide stimulates the proliferation of mouse spleen lymphocytes and enhances cellular immune responses. It is used for research on immunomodulation, food-derived bioactive peptides, and potential functional food ingredients. For research use only; not for human therapy.
Biological Activity I Assay Protocols (From Reference)
Targets
The peptide targets immune cells, specifically lymphocytes (T cells and B cells). It acts as an immunostimulatory agent, promoting lymphocyte proliferation, possibly by activating signaling pathways such as MAPK/ERK or by modulating cytokine production. It does not target a specific receptor; rather, it may interact with cell surface molecules (e.g., pattern recognition receptors or chemokine receptors) to enhance immune function. The peptide is derived from casein, and similar peptides have been shown to increase phagocytosis of macrophages, stimulate natural killer (NK) cell activity, and increase secretion of IL-2 and IFN-gamma. The mechanism is likely via direct interaction with immune cell membranes or specific receptors (e.g., formyl peptide receptor-like). It operates within the immunomodulation pathway.
ln Vitro
In vitro, alphas1-CN f(143-149) acetate stimulates the proliferation of mouse spleen lymphocytes. A typical assay: isolate splenocytes from BALB/c mice, resuspend in RPMI-1640 with 10% FBS, 2-mercaptoethanol. Seed cells in 96-well plates (2×10⁵ cells/well). Add the peptide at concentrations of 0.1, 1, 10, 50, 100, 200 ug/mL (prepare in PBS, DMSO not used). Incubate at 37degC in 5% CO2 for 48-72 h. Add [3H]-thymidine (1 uCi/well) for the last 16-18 h, harvest, and measure thymidine incorporation. Alternatively, use MTT or CellTiter-Glo. Stimulation index (SI) = (CPM with peptide)/(CPM with medium). The peptide increases proliferation in a concentration-dependent manner, with maximal effect at 50-100 ug/mL (SI of 2-5 fold). It also increases cytokine secretion: collect supernatants and measure IL-2 and IFN-gamma by ELISA. No cytotoxicity observed up to 200 ug/mL. Positive control: concanavalin A (ConA, 2.5 ug/mL). Negative control: medium only. All experiments in triplicate.
ln Vivo
No in vivo activity data are provided. The peptide is from milk protein and has been studied for immune-enhancing effects in animal models. In a typical study, mice may be orally administered the peptide (0.1-10 mg/kg) daily for 7-14 days, then splenocytes isolated and ex vivo proliferation measured. It may also enhance resistance to infection (e.g., Candida, Listeria) in mouse models. Specific protocols not available. For research use only.
Enzyme Assay
Not applicable. The peptide acts on lymphocytes via direct interaction; the molecular target is not an enzyme. Non-cellular receptor binding assays could be performed using radiolabeled peptide and lymphocyte membranes, but such assays are not standard for this product. The primary characterization is through cell proliferation assays.
Cell Assay
For in vitro splenocyte proliferation assay, as described above. Additionally, for macrophage activation, culture RAW264.7 macrophages with peptide (10-200 ug/mL) for 24 h, measure NO production (Griess reagent) and phagocytosis of FITC-labeled E. coli or latex beads by flow cytometry. No specific enzyme inhibition assays.
Animal Protocol
No published in vivo protocols. A typical study could involve oral gavage of the peptide to C57BL/6 mice (10-100 mg/kg) daily for 7 days, then sacrifice, harvest spleen, and measure ex vivo T cell proliferation to ConA. Another model: immunize mice with ovalbumin, co-administer peptide, and measure antibody titers. Not performed in source. For research only.
ADME/Pharmacokinetics
As a heptapeptide, it is susceptible to proteolytic degradation in the gastrointestinal tract. Oral bioavailability likely low; it may exert local effects on gut-associated lymphoid tissue (GALT). Half-life in plasma short (<30 min). Storage: lyophilized at -20degC. Solubility: water, PBS.
Toxicity/Toxicokinetics
No toxicity data. At concentrations up to 200 ug/mL, no cytotoxicity. Generally considered safe as a milk-derived peptide. Standard precautions: use PPE.
References

[1]. "Novel casein-derived peptides with antihypertensive activity." International dairy journal 19.10 (2009): 566-573.

Additional Infomation
Sequence: Gly-Lys-Leu-Lys-Lys-Ile-Asn (GKLKKIN). Molecular weight approx. 800. Purity >95% by HPLC. Acetate salt. Research areas: immunomodulation, functional food. Not for human use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C46H59N7O12.XC2H4O2
Molecular Weight
902.00 (free base)
Related CAS #
αs1-CN f(143–149)
Sequence
Ala-Tyr-Phe-Tyr-Pro-Glu-LeuAYFYPEL
Appearance
White to off-white solid powder
HS Tariff Code
2934.99.9001
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)
Solubility Data
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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