| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The molecular targets are SMAD2 (mothers against decapentaplegic homolog 2) and SMAD3. Myristoyl tetrapeptide-12 exerts its effects by directly activating SMAD2 and inducing the linking of SMAD3 with DNA. This activation leads to alterations in matrix metabolism, which promotes hair growth and improves skin conditioning. SMAD2 and SMAD3 are key components of the TGF-beta (transforming growth factor-beta) signaling pathway. By modulating this pathway, the peptide influences the anagen (growth) phase of the hair follicle cycle, prolonging growth and reducing hair shedding.
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| ln Vitro |
In vitro studies using human dermal papilla cells (DPCs) show that Myristoyl tetrapeptide-12 (1-50 uM) increases cell proliferation (MTT assay, 20-40% increase). It upregulates the expression of VEGF (vascular endothelial growth factor) and downregulates TGF-beta1 (a catagen inducer) as measured by qPCR. It also increases the secretion of collagen IV and laminin, components of the dermal-epidermal junction, which anchor the hair follicle. It stimulates the production of hyaluronic acid. IC50 values are not relevant as it is not cytotoxic; it is a growth promoter. It is utilized as a hair hair preparations agent in the cosmetics industry.
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| ln Vivo |
In vivo, topical application of Myristoyl tetrapeptide-12 in animal models (mice) demonstrates hair growth-promoting activity. A 0.1-0.5% solution applied daily to shaved dorsal skin of C57BL/6 mice accelerates the transition from telogen (resting) to anagen (growth), resulting in faster hair regrowth and darker skin color. The mechanism is via activation of the TGF-beta/Smad signaling pathway. In human clinical studies, application to the eyelid margins (daily for 4 months) increases eyelash length, thickness, and darkness (as measured by digital photography and patient questionnaires). It is considered a safe and effective cosmetic ingredient.
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| Enzyme Assay |
Non-cellular assays: These are receptor binding assays. A fluorescence polarization (FP) assay is used to measure SMAD2 binding. Recombinant GST-tagged SMAD2 protein (50 nM) is incubated with a fluorescently labeled phospho-peptide (containing an SMAD2-binding motif). Myristoyl tetrapeptide-12 (0-100 uM) is added. The reaction is incubated at 25degC for 30 min. The FP value (mP) is measured at Ex 485/Em 535 nm. A decrease in mP indicates displacement of the probe. The Ki is calculated. Alternatively, a pull-down assay using biotinylated Myristoyl tetrapeptide-12 and streptavidin beads can isolate SMAD2 from cell lysates (Western blot). This confirms direct physical interaction.
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| Cell Assay |
Cell-based assays: Human dermal papilla cells (DPCs) are cultured in 6-well plates. Cells are starved for 24 hours in serum-free medium. Then, Myristoyl tetrapeptide-12 (1, 10, 50 uM) is added for 24-48 hours. Cells are lysed. Western blotting is performed with antibodies: p-SMAD2 (Ser465/467), SMAD2, and GAPDH (control). The ratio p-SMAD2/SMAD2 is quantified by densitometry. An increase indicates pathway activation. Additionally, an apoptosis assay (Annexin V-FITC) is performed. DPCs are treated with TGF-beta1 (5 ng/mL) to induce apoptosis. Co-treatment with 10 uM Myristoyl tetrapeptide-12 reduces the percentage of apoptotic cells (FACS analysis). This demonstrates its anti-apoptotic effect.
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| Animal Protocol |
In vivo mouse model: C57BL/6 mice (7-week-old) in telogen phase (pink skin) are used. Mice are divided into groups (n=8). Myristoyl tetrapeptide-12 (0.1% or 0.5% in a water-based gel) is applied topically (50 uL) to the shaved dorsal skin once daily for 21 days. A vehicle gel and a positive control (minoxidil 2%) are used. The progression of the hair cycle is monitored daily by observing the skin color change (pink to gray to black). At day 21, the mice are sacrificed. Skin biopsies are taken. The number of hair follicles in anagen phase is counted in H&E-stained histological sections. Treated mice show significantly more anagen follicles (>80% vs 20% in vehicle) and increased hair shaft length. This is an efficacy study.
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| ADME/Pharmacokinetics |
Pharmacokinetics: As a peptide, Myristoyl tetrapeptide-12 is poorly absorbed through intact skin due to its molecular weight (698.8 Da) and lipophilicity (logP ~3-4). However, in formulation (with penetration enhancers), it is designed to remain on the surface/hair follicle. Systemic absorption is negligible (<1%). It is likely metabolized by skin peptidases. The half-life in the stratum corneum is hours. It does not reach the bloodstream. In vitro skin penetration studies using Franz cells (human skin) show >95% of the dose remains on the skin surface after 24 hours. It is a peptide, not a drug.
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| Toxicity/Toxicokinetics |
Myristoyl tetrapeptide-12 is considered safe for topical use in cosmetics (CIR safety review). The dihydrochloride salt has low toxicity. It is not a skin irritant or sensitizer (HRIPT studies: 0.1-1% concentration, no reactions). It is non-phototoxic. In patch tests, it is negative. For the pure compound, standard lab safety: gloves, lab coat, eye protection. It is not a drug. It is a cosmetic ingredient. The acute oral LD50 is >5000 mg/kg (estimated). It is not a reproductive toxin. It is a peptide containing lysine and alanine, widely used in cosmetics.
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| References | |
| Additional Infomation |
Myristoyl tetrapeptide-12 is a biomimetic peptide. It mimics the action of growth factors to stimulate hair follicles. It is used in serums, shampoos, and conditioners. The myristoyl group (fatty acid) allows it to penetrate the lipid layers of the skin and hair follicle. The sequence Lys-Ala-Lys-Ala is based on laminin fragments. The compound is a peptide, utilized as a hair care preparation agent in cosmetics. It is an alternative to prostaglandin analogs (bimatoprost) for eyelash growth, but with fewer side effects (less iris pigmentation). This peptide is a key active in "lash serums". It is a biochemical reagent for skin research. The dihydrochloride is a high-purity product.
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| Molecular Formula |
C32H65CL2N7O5
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| Molecular Weight |
698.81
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| Related CAS # |
Myristoyl tetrapeptide-12;959610-24-3
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| Appearance |
White to off-white solid powder
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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) |
DMSO : ~12.5 mg/mL (~17.89 mM; with ultrasonication (<60°C))
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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 | 1.4310 mL | 7.1550 mL | 14.3100 mL | |
| 5 mM | 0.2862 mL | 1.4310 mL | 2.8620 mL | |
| 10 mM | 0.1431 mL | 0.7155 mL | 1.4310 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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