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| Other Sizes |
| Targets |
Casein hydrolysate is a mixture of bioactive peptides that target multiple pathways. The primary target is angiotensin‑converting enzyme (ACE), a key enzyme in the renin‑angiotensin system that converts angiotensin I to the vasoconstrictor angiotensin II and degrades the vasodilator bradykinin. By inhibiting ACE, casein hydrolysate peptides lower blood pressure. Casein hydrolysate also contains immunomodulatory peptides that may act on immune cells (e.g., T lymphocytes, macrophages) to enhance immune function, as evidenced by increased ConA‑induced IL‑2 production. Additionally, some peptides exhibit metal ion chelation, free radical scavenging, and antibacterial activities.
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| ln Vitro |
Casein hydrolysate contains peptides that inhibit angiotensin‑converting enzyme (ACE), leading to reduced conversion of angiotensin I to angiotensin II and decreased degradation of bradykinin, resulting in vasodilation and blood pressure reduction. It also increases cellular glutathione and catalase levels, enhancing the cellular antioxidant defense system. Casein hydrolysate enhances ConA‑induced IL‑2 production, indicating immunomodulatory activity. It also exhibits metal ion chelation, free radical scavenging (antioxidant), antibacterial, and mineral absorption‑promoting effects. No specific IC50 values for individual peptides are reported, as it is a complex mixture.
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| ln Vivo |
In vivo, casein hydrolysate is an orally effective mixture of bioactive peptides that lowers blood pressure by inhibiting angiotensin‑converting enzyme (ACE) and reducing bradykinin degradation. It has been studied in randomized controlled trials for its effects on cardiovascular risk factors. The mixture increases cellular glutathione and catalase levels, enhances ConA‑induced IL‑2 production (indicating immunomodulation), and exhibits metal chelation, free radical scavenging, antibacterial, and mineral absorption‑promoting effects. The peptide mixture is derived from the enzymatic hydrolysis of casein.
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| Enzyme Assay |
The bioactive peptides in casein hydrolysate are not evaluated in individual enzyme/receptor binding assays as a mixture. The ACE inhibitory activity is measured by standard in vitro assays using purified ACE and a synthetic substrate (e.g., hippuryl‑L‑histidyl‑L‑leucine, HHL). Casein hydrolysate is incubated with ACE and the substrate. After incubation, the hippuric acid product is extracted with ethyl acetate and measured by spectrophotometry at 228 nm. The IC50 of the hydrolysate is calculated. The peptide composition is analyzed by HPLC‑MS/MS.
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| Cell Assay |
For cellular assays, immune cells (e.g., splenocytes, peripheral blood mononuclear cells) are isolated and seeded in 96‑well plates. Cells are treated with casein hydrolysate at concentrations of 0.1-1000 ug/mL for 24-72 hours. Cell proliferation is measured by [3H]‑thymidine incorporation or MTT assay. Cytokine production (IL‑2, IFN‑gamma, IL‑4, IL‑10) is measured by ELISA. For antioxidant assays, cells are treated with the hydrolysate, then exposed to oxidative stress (e.g., H2O2). Intracellular glutathione and catalase levels are measured by colorimetric assays, and reactive oxygen species (ROS) are measured by DCFH‑DA fluorescence.
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| Animal Protocol |
For in vivo evaluation of antihypertensive effects, male spontaneously hypertensive rats (SHRs) are used. Casein hydrolysate is administered orally (by gavage) at doses of 100-1000 mg/kg. Systolic blood pressure (SBP) is measured by the tail‑cuff method at various time points (0, 2, 4, 6, 8, 24 h) after administration. For immunomodulatory studies, mice are treated orally with casein hydrolysate (100-1000 mg/kg) for 7-14 days, then splenocytes are harvested, and ex vivo T cell proliferation and cytokine production are measured. For antibacterial studies, mice infected with bacteria are treated with the hydrolysate, and bacterial load and survival are assessed. No specific protocols are described.
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| ADME/Pharmacokinetics |
Casein hydrolysate (CAS 65072-00-6) is a pale yellow to light brown, free‑flowing powder, slightly hygroscopic. It is soluble in water, yielding a clear, yellow to brownish‑yellow solution. The amino acid profile: Ala 2.8%, Arg 3.6%, Asp 6.3%, Cystine 0.3%, Glu 21.1%, Gly 2.2%, His 2.7%, Ile 5.6%, Leu 8.4%, Lys 7.5%, Met 2.7%, Phe 4.6%, Pro 9.9%, Ser 5.6%, Thr 4.2%, Trp 1.1%, Tyr 6.1%, Val 5.0%. For storage, the powder should be kept at 4degC or -20degC, sealed and protected from moisture. For in vitro use, stock solutions in water (10-100 mg/mL) can be prepared and stored at -20degC for up to 1 month. No detailed PK parameters are reported for the complex mixture.
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| Toxicity/Toxicokinetics |
Casein hydrolysate is generally recognized as safe (GRAS) as a food ingredient. It has low toxicity and is well‑tolerated when consumed orally. In randomized controlled trials, casein hydrolysate has been shown to reduce blood pressure without significant adverse effects. As a research‑grade product, it is not intended for therapeutic use in its research form. Standard laboratory safety precautions for handling powders should be followed.
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| References | |
| Additional Infomation |
Casein hydrolysate (also known as casamino acids) is a complete enzymatic or acid hydrolysate of casein, the primary protein in milk. It is a rich source of amino acids and short peptides. It is widely used as a nutrient supplement in microbial culture media and as a source of bioactive peptides for research into hypertension, immunomodulation, and antioxidant effects. The ACE‑inhibitory peptides in casein hydrolysate, such as the tripeptides VPP (Val‑Pro‑Pro) and IPP (Ile‑Pro‑Pro), are well‑studied antihypertensive peptides. Casein hydrolysate is for research use only and has not received regulatory approval as a drug.
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| Exact Mass |
539.28
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|---|---|
| CAS # |
65072-00-6
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| PubChem CID |
57397142
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
823.0±65.0 °C at 760 mmHg
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| Flash Point |
451.6±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
-2.45
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
760
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| Defined Atom Stereocenter Count |
15
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| SMILES |
CN[C@H]1[C@H](C2C(C[C@H]([C@H](O2)O[C@@H]3[C@H](C[C@H]([C@@H]([C@H]3O)O)N)N)N)O[C@@H]1O[C@@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)N)O)O)O
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| InChi Key |
XZNUGFQTQHRASN-PSDDYZKFSA-N
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| InChi Code |
InChI=1S/C21H41N5O11/c1-26-11-14(30)18-8(33-20(11)37-21-16(32)13(29)10(25)9(4-27)34-21)3-7(24)19(36-18)35-17-6(23)2-5(22)12(28)15(17)31/h5-21,26-32H,2-4,22-25H2,1H3/t5-,6+,7-,8?,9-,10-,11+,12+,13+,14-,15-,16-,17-,18?,19+,20-,21-/m1/s1
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| Chemical Name |
(2R,3R,4S,5S,6S)-5-amino-2-[[(2R,3S,4R,6S,7R)-7-amino-6-[(1R,2R,3S,4R,6S)-4,6-diamino-2,3-dihydroxycyclohexyl]oxy-4-hydroxy-3-(methylamino)-2,3,4,4a,6,7,8,8a-octahydropyrano[3,2-b]pyran-2-yl]oxy]-6-(hydroxymethyl)oxane-3,4-diol
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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 |
| 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.) |
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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