| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
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| Targets |
Vascular permeability-related targets (mechanism associated with reducing extravasation of fluid and proteins) [3]
- Angiotensin-converting enzyme (ACE)-like activity modulation (contributes to edema reduction) [3] |
|---|---|
| ln Vitro |
Angiotensin-converting enzyme 1 (ACE-1) activity is inhibited by acetyl tetrapeptide-5 (100 μg/mL) [1].
Protection against H2O2-induced premature senescence in human skin fibroblasts Pretreatment with Acetyl tetrapeptide-5 (100 μM) for 24 hours significantly increased cell viability (MTT assay) by 35.2% compared to H2O2-treated control cells. It reduced intracellular reactive oxygen species (ROS) levels by 42.1% (DCFH-DA staining) and malondialdehyde (MDA) content by 38.7%, while increasing superoxide dismutase (SOD) activity by 51.3% and glutathione (GSH) levels by 47.6%. The peptide also upregulated mRNA expression of collagen type I (COL1A1) by 2.3-fold and downregulated senescence-associated β-galactosidase (SA-β-gal) activity by 58.9% (histochemical staining) [1] - Reduction of vascular endothelial cell permeability In human umbilical vein endothelial cells (HUVECs), Acetyl tetrapeptide-5 (50–200 μM) dose-dependently decreased the permeability of FITC-dextran (40 kDa) across the cell monolayer. At 100 μM, it inhibited permeability by 41.8% compared to the control group, indicating a role in stabilizing the endothelial barrier [3] - Modulation of extracellular matrix (ECM) components In human skin fibroblasts, Acetyl tetrapeptide-5 (100 μM) increased the synthesis of collagen type III (COL3A1) mRNA by 1.8-fold and reduced matrix metalloproteinase-1 (MMP-1) mRNA expression by 43.2% (qPCR analysis), as well as MMP-1 protein secretion by 39.5% (ELISA) [1] |
| ln Vivo |
Reduction of periorbital edema in animal models
In female rats with carrageenan-induced periorbital edema, topical application of Acetyl tetrapeptide-5 (0.1% w/w in cream formulation) twice daily for 3 days significantly reduced edema volume by 37.4% compared to the vehicle control. Measurement was performed using a digital plethysmometer, and histological analysis showed reduced interstitial fluid accumulation and decreased inflammatory cell infiltration in the periorbital tissue [3] - Improvement of skin firmness and reduction of under-eye puffiness in human clinical trials A 28-day randomized controlled trial involving 30 female volunteers (40–60 years old) showed that twice-daily topical application of a cream containing 0.05% Acetyl tetrapeptide-5 reduced under-eye puffiness by 21.3% (digital image analysis) and improved skin firmness around the orbital area by 18.7% (cutometer measurement). Self-assessment questionnaires indicated 73.3% of participants reported a noticeable reduction in under-eye bags [3] |
| Cell Assay |
H2O2-induced premature senescence assay in human skin fibroblasts
Human skin fibroblasts were cultured in complete medium until 70–80% confluence, then serum-starved for 24 hours. Cells were pretreated with Acetyl tetrapeptide-5 at concentrations of 10, 50, 100 μM for 24 hours, followed by exposure to 200 μM H2O2 for 2 hours to induce senescence. After 48 hours of recovery, cell viability was measured via MTT assay, ROS levels using DCFH-DA fluorescent probe, and MDA, SOD, GSH levels via colorimetric kits. SA-β-gal staining was performed to identify senescent cells, and qPCR was used to detect COL1A1, COL3A1, and MMP-1 mRNA expression [1] - Vascular endothelial permeability assay in HUVECs HUVECs were seeded on transwell inserts coated with Matrigel and cultured until a confluent monolayer was formed. Acetyl tetrapeptide-5 was added to the apical chamber at 50, 100, 200 μM and incubated for 24 hours. FITC-dextran (40 kDa) was then added to the apical chamber, and after 2 hours, the fluorescence intensity of the basolateral chamber was measured using a microplate reader to calculate permeability coefficients [3] |
| Animal Protocol |
Periorbital edema model in rats
Female Sprague-Dawley rats (200–250 g) were acclimated for 7 days before the experiment. Periorbital edema was induced by subcutaneous injection of 0.1 mL carrageenan (1% w/v) into the right orbital region. Acetyl tetrapeptide-5 was formulated into a cream at 0.1% w/w, and 0.05 g of the cream was topically applied to the edematous area twice daily (morning and evening) for 3 days. The vehicle control group received the same cream without the peptide. Edema volume was measured before induction and at 24, 48, 72 hours after the first application using a digital plethysmometer. At the end of the experiment, rats were euthanized, and periorbital tissue samples were collected for histological analysis [3] |
| References | |
| Additional Infomation |
See also: Acetyl Octapeptide-3; Acetyl Tetrapeptide-5 (component).
Mechanism of Action Acetyl Tetrapeptide-5 exerts its anti-edema effect by modulating vascular permeability, possibly by inhibiting the activity of enzymes involved in vasodilation and fluid exudation (e.g., ACE-like enzymes). It also exhibits antioxidant and anti-aging properties in skin fibroblasts by scavenging reactive oxygen species (ROS), reducing damage caused by oxidative stress, and regulating the synthesis and degradation of the extracellular matrix (ECM) [1, 3]. -Cosmetic Applications This peptide is a key active ingredient in anti-aging and eye care cosmetics, particularly effective in reducing puffiness, edema, and improving the firmness of the skin around the eyes. It is typically formulated as creams, serums, and gels at concentrations ranging from 0.05% to 0.1% w/w [2, 3] - Synergistic Effects with Other Peptides When used in combination with other cosmeceutical peptides such as palmitoyl tripeptide-5 and copper tripeptide-1, acetyl tetrapeptide-5 enhances its efficacy in reducing signs of skin aging, including fine lines and wrinkles, through a mechanism of action that synergistically promotes collagen synthesis and reduces oxidative stress [1, 2] |
| Molecular Formula |
C20H28N8O7
|
|---|---|
| Molecular Weight |
492.485723495483
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| Exact Mass |
492.208
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| CAS # |
820959-17-9
|
| PubChem CID |
11620163
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
1237.3±65.0 °C at 760 mmHg
|
| Flash Point |
702.1±34.3 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.611
|
| LogP |
-3.79
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
35
|
| Complexity |
768
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
[C@@H](NC(=O)CCNC(=O)C)(C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CC1NC=NC=1)CC1NC=NC=1
|
| InChi Key |
ROTFCACGLKOUGI-JYJNAYRXSA-N
|
| InChi Code |
InChI=1S/C20H28N8O7/c1-11(30)23-3-2-17(31)26-14(4-12-6-21-9-24-12)18(32)28-16(8-29)19(33)27-15(20(34)35)5-13-7-22-10-25-13/h6-7,9-10,14-16,29H,2-5,8H2,1H3,(H,21,24)(H,22,25)(H,23,30)(H,26,31)(H,27,33)(H,28,32)(H,34,35)/t14-,15-,16-/m0/s1
|
| Chemical Name |
(3-acetamidopropanoyl)-L-histidyl-L-seryl-L-histidine
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| Synonyms |
Eyeseryl; Ac-beta-ala-his-ser-his-oh; Acetyl Tetrapeptide-5
|
| 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 (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) |
DMSO : ~25 mg/mL (~50.76 mM)
|
|---|---|
| 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 | 2.0305 mL | 10.1525 mL | 20.3050 mL | |
| 5 mM | 0.4061 mL | 2.0305 mL | 4.0610 mL | |
| 10 mM | 0.2030 mL | 1.0152 mL | 2.0305 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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