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Acetyl tetrapeptide-15

Alias: SkinasensylAcetyl tetrapeptide-15
Cat No.:V8583 Purity: ≥98%
Acetyl tetrapeptide-15 is a synthetic peptide used in cosmetics for sensitive skin.
Acetyl tetrapeptide-15
Acetyl tetrapeptide-15 Chemical Structure CAS No.: 928007-64-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Acetyl tetrapeptide-15 is a synthetic peptide used in cosmetics for sensitive skin. Acetyl tetrapeptide-15 is developed from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective analgesia. Acetyl tetrapeptide-15 increases neuronal excitability thresholds in μ-opioid receptors via endorphin-like pathways, reducing inflammatory, chronic and neuropathic pain resulting from cutaneous hyperresponsiveness.
Acetyl tetrapeptide-15 (CAS#: 928007-64-1), also known as Skinasensyl, is a synthetic peptide used in cosmetic and dermatological formulations for sensitive skin. It is derived from endorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid receptor agonist with selective antinociceptive effects. Its molecular formula is C34H39N5O6, and its molecular weight is 613.7. The peptide is designed to reduce skin sensitivity and discomfort by modulating the skin's response to external irritants. It raises the excitatory threshold of μ-opioid receptor neurons via an endorphin-like pathway, decreasing skin hyperreactivity and reducing inflammation.
Biological Activity I Assay Protocols (From Reference)
Targets
Acetyl tetrapeptide-15 targets the μ-opioid receptor, a G protein-coupled receptor that is part of the endogenous opioid system. The peptide is derived from endorphin-2, a natural endogenous ligand for this receptor. By acting as an agonist at the μ-opioid receptor, it raises the excitatory threshold of sensory neurons. This mechanism reduces the skin's hyperreactivity to external stimuli, thereby decreasing the sensation of discomfort, redness, and inflammation associated with sensitive skin. The μ-opioid receptor pathway is thus a key target for managing neurogenic inflammation and skin sensitivity.
ln Vitro
In vitro, Acetyl tetrapeptide-15 has been shown to reduce the release of pro-inflammatory mediators from skin cells. It modulates the skin’s response to external irritants by decreasing neurogenic inflammation. The peptide works by binding to μ-opioid receptors on sensory nerve endings in the skin, which inhibits the release of substance P and calcitonin gene-related peptide (CGRP), two neuropeptides involved in the transmission of pain and the initiation of inflammatory responses. This results in a reduction of redness, itching, and other signs of skin irritation. The peptide's activity is specific to the μ-opioid receptor pathway, making it an effective agent for soothing sensitive skin.
ln Vivo
In vivo, Acetyl tetrapeptide-15 has been demonstrated to improve skin tolerance and reduce sensitivity in human clinical studies (typically conducted as part of cosmetic product testing). It has been shown to decrease skin reactivity to chemical and physical irritants, such as capsaicin or lactic acid, in patch test models. The peptide helps to alleviate discomfort caused by environmental factors and reduces the symptoms of sensitive skin, including redness, stinging, and itching. It is often included in leave-on skincare products at recommended dosages of 0.2-6%.
Enzyme Assay
Non-cellular in vitro assays for Acetyl tetrapeptide-15 typically involve receptor binding studies. A standard protocol uses membrane preparations from cells expressing recombinant human μ-opioid receptors. The membranes are incubated with a radiolabeled ligand, such as [³H]DAMGO (a selective μ-opioid agonist), and varying concentrations of the peptide. Non-specific binding is determined in the presence of an excess of unlabeled naloxone. After incubation, the reaction is terminated by rapid filtration, and the radioactivity bound to the membranes is measured. The IC50 or Ki values are calculated from the competition curves.
Cell Assay
Cellular assays for Acetyl tetrapeptide-15 are performed using neuronal cell lines that express μ-opioid receptors, such as SH-SY5Y neuroblastoma cells. Cells are treated with the peptide at various concentrations for a period of time (e.g., 24 hours). To assess receptor activation, downstream signaling pathways such as the inhibition of adenylyl cyclase or the activation of MAPK/ERK can be measured. Alternatively, the release of substance P or CGRP from sensory neurons can be measured in response to stimulation with capsaicin, and the inhibitory effect of the peptide on neuropeptide release can be determined.
Animal Protocol
In vivo animal studies for Acetyl tetrapeptide-15 are limited, as it is primarily a cosmetic ingredient. However, for preclinical evaluation, it can be tested in animal models of skin irritation. For example, mice or rats can be treated topically with an irritant (e.g., arachidonic acid or phorbol ester) to induce ear edema. The peptide is then applied to the treated area, and the reduction in ear swelling is measured after a specified time (e.g., 4-6 hours). This model assesses the anti-inflammatory and soothing effects of the peptide in vivo.
ADME/Pharmacokinetics
Acetyl tetrapeptide-15 is a synthetic peptide with a molecular weight of 613.7. It is a solid powder that is typically stored at -20°C, protected from light. Its solubility is not extensively detailed, but as a peptide, it is expected to be soluble in water and suitable for formulation in aqueous cosmetic vehicles. The peptide is designed for topical application, and its pharmacokinetics are not typically characterized in terms of systemic absorption, as it is intended to act locally in the skin. However, its effects are mediated through receptor binding on cutaneous nerve endings.
Toxicity/Toxicokinetics
Acetyl tetrapeptide-15 is considered to have a very favorable safety profile for topical use. It is non-irritating and well-tolerated by the skin. It is not intended for systemic use, and systemic toxicity is not a concern due to its topical application. It is not a drug and is not approved for therapeutic use; it is classified as a cosmetic ingredient. Standard safety assessments for cosmetic ingredients have been performed, and it is considered safe for use in cosmetic products at recommended concentrations (0.2-6%).
References

[1]. Usage of Synthetic Peptides in Cosmetics for Sensitive Skin. Pharmaceuticals (Basel). 2021;14(8):702.

Additional Infomation
Acetyl tetrapeptide-15, marketed under the trade name Skinasensyl, is a well-known active ingredient in the cosmetics industry. It is designed to address the needs of sensitive skin by mimicking the natural endorphin pathway to calm skin reactivity. The peptide is often used in anti-redness, anti-itching, and soothing formulations. It is not a pharmaceutical and has no clinical trials or regulatory approval for medical use. Its value lies in its ability to provide a biomimetic approach to skincare, helping to restore the skin's natural tolerance threshold.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C34H39N5O6
Molecular Weight
613.71
Exact Mass
613.29
CAS #
928007-64-1
PubChem CID
16657387
Appearance
White to off-white solid powder
Density
1.3±0.1 g/cm3
Boiling Point
1055.3±65.0 °C at 760 mmHg
Flash Point
592.0±34.3 °C
Vapour Pressure
0.0±0.3 mmHg at 25°C
Index of Refraction
1.617
LogP
2.72
Hydrogen Bond Donor Count
5
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
13
Heavy Atom Count
45
Complexity
1020
Defined Atom Stereocenter Count
4
SMILES
CC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N
InChi Key
BSXFOBDOGHFWOC-KRCBVYEFSA-N
InChi Code
InChI=1S/C34H39N5O6/c1-22(40)36-29(21-25-14-16-26(41)17-15-25)34(45)39-18-8-13-30(39)33(44)38-28(20-24-11-6-3-7-12-24)32(43)37-27(31(35)42)19-23-9-4-2-5-10-23/h2-7,9-12,14-17,27-30,41H,8,13,18-21H2,1H3,(H2,35,42)(H,36,40)(H,37,43)(H,38,44)/t27-,28-,29-,30-/m0/s1
Chemical Name
(2S)-1-[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide
Synonyms
SkinasensylAcetyl tetrapeptide-15
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~162.95 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6294 mL 8.1472 mL 16.2943 mL
5 mM 0.3259 mL 1.6294 mL 3.2589 mL
10 mM 0.1629 mL 0.8147 mL 1.6294 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.

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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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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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