Biotinoyl Tripeptide-1 is an innovative tripeptide compound formed by chemically combining vitamin H (biotin) with a signaling copper peptide (GHK, a Matrikine). It usually exists in the form of white powder, or can be pre dissolved in solvents to make liquid solutions for use in cosmetics and personal care products. Mainly used to promote hair growth, prevent hair loss, improve hair health, and support skin repair and regeneration. Composed of biotin and three amino acid residues (glycine, histidine, lysine). Biotin, also known as vitamin H or vitamin B7, is a water-soluble vitamin that is crucial for human growth, development, and normal bodily functions, especially playing an indispensable role in the metabolism of fats and proteins. GHK tripeptide is a short peptide with biological activity that can bind with biotin to form a unique functional hair growth peptide.
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Biotinoyl Tripeptide-1 COA
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| Certificate of Analysis | ||
| Compound name | Biotinoyl tripeptide-1 | |
| Grade | Pharmaceutical grade | |
| CAS No. | 299157-54-3 | |
| Quantity | 15g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202512090055 | |
| MFG | Dec 9th 2025 | |
| EXP | Dec 8th 2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.47% |
| Loss on drying | ≤1.0% | 0.55% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.90% |
| Single impurity | <0.8% | 0.26% |
| Total microbial count | ≤750cfu/g | 70 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400 ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula | C24H38N8O6S | |
| Exact Mass | 566.26 | |
| Molecular Weight | 566.68 | |
| m/z | 566.26 (100.0%),567.27(26.0%),568.26(4.5%),568.27(3.2%),567.26(3.0%),568.27(1.2%),569.26(1.2%) | |
| Elemental Analysis | C,50.87;H,6.76;N,19.77;O,16.94;S,5.66 | |
Biotinoyl Tripeptide-1 is a biologically active molecule formed by the covalent binding of biotin (vitamin B7) with glycyl-L-histidyl-L-lysine (GHK) tripeptide. Its molecular formula is C24H38N8O6S, with a molecular weight of 566.67. It appears as a white to off white powder with a purity of over 99%. This molecule has attracted much attention due to its significant effects in the field of hair health, but there are significant differences between its in vitro and in vivo effects, posing challenges to scientific research and clinical applications.
Molecular mechanism: synergistic effect of biotin and GHK
Its activity originates from the synergistic effect of biotin and GHK tripeptide:
Biotin is a key coenzyme in keratin synthesis, involved in the metabolism of fatty acids, glucose, and amino acids. In hair follicles, biotin promotes fatty acid synthesis by activating acetyl CoA carboxylase (ACC), providing an energy foundation for hair growth. In addition, biotin can enhance the antioxidant capacity of hair follicle cells and reduce UV induced DNA damage.
The binding of biotin to GHK significantly enhances the stability of the molecule (11 times higher than GHK alone) and hair follicle targeting. Biotin acts as a "navigation molecule" to guide GHK into hair follicle cells, and GHK directly acts on key targets of the hair follicle growth cycle through its biological activity.
The function of GHK tripeptide
GHK tripeptides have multiple biological activities:
Cell proliferation promotion: By activating the MAPK/ERK signaling pathway, it stimulates the proliferation of dermal papilla cells (DPC). In vitro experiments showed that the cell proliferation rate reached 148.24% at a concentration of 0.625%.
Antioxidant defense: Chelate copper ions (Cu ² ⁺), inhibit their catalytic reaction to generate reactive oxygen species (ROS), and reduce oxidative stress damage to hair follicles.
Anti amyloid protein aggregation: Inhibiting the production and aggregation of carbonylated amyloid beta protein (A β) may be achieved by regulating metal ion balance.
In vitro studies: mechanism validation and dose-response analysis
Proliferation effect: In human dermal papilla cells (HHDPCs) cultured in vitro, after treatment with 0.625% and 1.25% concentrations of the substance for 72 hours, the cell proliferation rates reached 148.24% and 143.59%, respectively, with no significant difference compared to the positive control minoxidil (150.12%). But the proliferation rate dropped sharply to 102.31% at a concentration of 2.5%, indicating a dose-dependent saturation effect.
Antioxidant mechanism: By chelating Cu ² ⁺, it can inhibit the oxidation of ascorbic acid (ASC) induced by Cu-A β complex and reduce ROS generation. In the A β 1-16 carbonylation model induced by acrolein, the inhibition rate of A β aggregation reached 65% at a concentration of 20 μ M, indicating its neuroprotective effect through metal ion regulation.
Molecular Interaction: Streptomycin Binding and Copper Chelation
Streptomycin binding: The affinity of this substance for streptavidin (IC ₅₀=30 μ M) is significantly higher than that of free biotin (IC ₅₀=1.2 μ M), which may be related to its spatial conformation optimization. However, this high affinity may be limited in vivo due to the presence of biological barriers such as the stratum corneum of the skin.
Copper chelation ability: GHK tripeptides can efficiently chelate Cu ² ⁺ (Kd=10 ⁻¹ ² M) through the imidazole group of histidine residues, forming stable Cu GHK complexes. This chelation can completely inhibit the ASC oxidation catalyzed by Cu ² ⁺ in vitro, but the dynamic equilibrium and competitive binding of copper ions need to be considered in vivo.
In vivo effects: clinical translation and limitations
Hair density increase: a clinical trial of essence containing 1% of the substance showed that the hair density increased by 29% after 16 weeks, and the proportion of hair in the growth period increased by 35% (hair follicle microscope detection). However, another study showed that only a 12% increase in density was observed at 8 weeks, suggesting individual differences in onset time.
Growth cycle regulation: It can improve the hair cycle by prolonging the hair growth period (Anagen) and shortening the rest period (Telogen). Animal experiments have shown that local application can increase the expression of hair follicle stem cell markers (such as CD34, K15), but the specific molecular pathways (such as Wnt/β - catenin) have not been fully elucidated.
Safety assessment: System exposure and local tolerance
Systemic toxicity: Even at high doses (0.6% biotin equivalent), the skin absorption rate is only about 10%, and biotin is rapidly metabolized into dihydrobiotin and biotin sulfide, with no risk of accumulation. In addition, biotin has not shown phototoxicity, mutagenicity, or teratogenicity and is suitable for long-term use.
Local irritation: Within the concentration range of 0.5% -3%, the substance did not cause adverse reactions such as erythema, itching, or flaking. However, some sensitive individuals may experience brief stinging sensations, which may be related to pH values (recommended 5.5-6.5) or formula compatibility.
Reasons for the disruption of in vitro studies and in vivo effects
Differences in bioavailability
Skin penetration barrier: In vitro experiments usually directly act on cells or tissues, while in vivo, it needs to penetrate the stratum corneum (thickness of about 10-20 μ m) and the epidermal dermal junction. Although the molecular weight of Biotinoyl Tripeptide-1 (566.67 Da) is less than the permeation threshold of 500 Da, its polarity (logP ≈ -2.5) may limit transmembrane transport.
Metabolic degradation: In the body, proteases (such as elastase and collagenase) and esterases in the skin may degrade the peptide or ester bonds of the substance, reducing its activity. The serum-free culture medium used in in vitro experiments cannot simulate this enzyme environment.
Dose effect differences
In vitro saturation effect: High concentrations (such as 2.5%) inhibit cell proliferation in vitro, which may be related to receptor saturation or non-specific binding. In the body, due to permeation limitations, the actual concentration reaching the hair follicle may be much lower than the effective concentration in vitro.
Internal dynamic balance: The concentration of copper ions in the body is regulated by various factors such as diet and disease status, and its copper chelation may be weakened due to copper deficiency. In addition, other antioxidant substances in the body, such as glutathione and vitamin C, may partially counteract their effects.
Limitations of the experimental model
Cell model simplification: In vitro experiments typically use a single cell type (such as HHDPCs), while in vivo hair follicles are a complex system of multiple cells (such as keratinocytes, melanocytes) and matrix components (such as collagen, hyaluronic acid). The effect of this substance may depend on intercellular interactions or the microenvironment of the matrix.
Animal model differences: The hair follicle cycle (about 20 days) in animal experiments (such as mice) is significantly different from that in humans (3-7 years), and the skin structure of animals (such as hair density and sebum secretion) is different from that in humans, which may lead to extrapolation bias of results.
Solutions and Future Directions
Delivery system optimization
Nanocarriers: By encapsulating Biotinoyl Tripeptide-1 with liposomes, polymer nanoparticles, or metal organic frameworks (MOFs), its skin permeability and stability can be improved. For example, liposome encapsulation can increase permeability by 3-5 times.
Micro needle technology: Directly delivered to the dermis layer through a soluble micro needle array, it can bypass the stratum corneum barrier and achieve precise targeting. Animal experiments have shown that microneedle delivery can increase drug concentration in hair follicles by 10 times.
Formula improvement
PH adjustment: Controlling the formula pH between 5.5-6.5 (close to skin pH) can reduce peptide charge rejection and improve permeability. Meanwhile, adding penetration enhancers such as propylene glycol and azone can further enhance the effect.
Stabilizer addition: Adding antioxidants (such as vitamin E) or protease inhibitors (such as EDTA) can prevent their degradation in the formula and extend the shelf life.
Combination therapy strategy
Combined with minoxidil: Minoxidil promotes hair follicle nutrition supply through vasodilation, while enhancing hair follicle vitality through cell proliferation and antioxidant effects. Preclinical studies have shown that the combination of 1% Biotinoyl Tripeptide and 2% Minoxidil can increase hair density by 42%, significantly better than monotherapy.
Combined with caffeine: Caffeine can inhibit 5 α - reductase, reduce dihydrotestosterone (DHT) production, and prevent hair follicle miniaturization. The combination of this substance and caffeine can synergistically improve androgenic alopecia, with animal experiments showing a 25% increase in hair diameter in the combined group.
In depth study of mechanisms
Single cell sequencing: Using single-cell RNA sequencing technology to analyze the differential effects of this substance on hair follicle stem cells, dermal papilla cells, and keratinocytes, revealing its specific pathways in regulating the hair cycle.
Organoid model: Constructing human hair follicle organoids to simulate the complex structure and function of hair follicles in vivo, which can more accurately evaluate their effects and toxicity.
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