Pentapeptide-3

1、 Product basic file

Chinese name: Pentapeptide-3 (also known as Villoside)

English name: Pentapeptide-3

CAS number: 135679-88-8 (free base form); 725232-44-0 (in the form of diacetate salt)

Molecular formula: C ₂₁ H ∝₇ N ₉ O ₅

Molecular weight: 495.58 g/mol

Amino acid sequence: H-Gly-Pro-Arg-Ala-NH ₂ (GPRPA-NH ₂)

Appearance specifications: White to off white solid powder, purity usually ≥ 95% (HPLC)

Solubility: Good water solubility due to its polar amino acid composition and charged nature of arginine residues

Storage conditions: Powder state sealed and protected from light, frozen storage at -20 ℃; After preparing the solution, it is recommended to store it for a short period of time at 2-8 ℃ and for a long period of time at -20 ℃ to avoid repeated freezing and thawing

2、 Core efficacy and mechanism of action

Pentapeptide-3 is a synthetic pentapeptide inspired by the neurotoxin Waglerin-1 protein in the venom of the Malaysian temple viper (Tropidolaemus wagleri). It is a biologically active pentapeptide fragment. Its core efficacy and mechanism of action are mainly reflected in the following dimensions:

Arrow like muscle relaxation and wrinkle resistance (core efficacy): Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) in muscles. It competes with acetylcholine to bind nAChRs on the postsynaptic membrane, occupying receptors but not activating ion channels, preventing Na ⁺ influx, inhibiting postsynaptic membrane depolarization, and thus blocking the transmission of nerve signals to muscles, producing a muscle relaxation effect similar to that of curare.

Rapid onset and long-lasting inhibition: In vitro studies have shown that treatment with pentapeptide-3 can reduce muscle contraction by up to 71% after 1 minute, and 58% of muscle fibers remain immobile after 2 hours, with a rapid and long-lasting effect.

Significant wrinkle reduction effect: Clinical studies have shown that using pentapeptide-3 twice a day for 28 consecutive days reduces wrinkle depth and skin roughness by nearly 50%. It can effectively improve facial expression lines such as forehead wrinkles, nasolabial folds, forehead wrinkles, and crow's feet.

Synergistic Enhancement with Acetyl Hexapeptide-8 (Argireline): An active control trial compared the anti wrinkle effects of 5% pentapeptide-3 (Leuphasyl) solution, 5% Argireline solution, and their 5%+5% combination. The results showed that the anti wrinkle effect of the two was comparable when used alone, but a significant synergistic effect was produced when used in combination, with a stronger anti wrinkle effect.

High safety and complete reversibility: Unlike botulinum toxin (which acts on the presynaptic membrane and inhibits acetylcholine release through enzymatic cleavage of SNARE protein), pentapeptide-3 acts on the postsynaptic membrane and achieves muscle relaxation through reversible competitive binding to receptors, without affecting normal expression, resulting in higher safety.

3、 Recommended addition ratio and application scenarios

Pentapeptide-3 formula has good compatibility and can be added to essence liquid, face cream, lotion, facial mask, eye cream and other formulations.

Recommended addition ratio:

Pure peptide activity concentration: 0.05% to 0.3% (calculated as pure peptide)

Recommended concentration of commodity solution: 3% to 10% (based on commodity solution)

Active ingredient dosage: 15-50 ppm

Anti wrinkle and firming essence/face cream: as the core active ingredient, it provides precise and light line care for expression lines such as eyebrow lines, decree lines, head lifting lines, puppet lines, etc., focusing on the concept of "smearing botulinum toxin like".

Eye care products: applied to eye creams, eye masks, etc., utilizing their significant wrinkle reducing ability to effectively improve crow's feet and dynamic wrinkles around the eyes.

Anti aging facial mask: Pentapeptide-3 facial mask is a classic application form, which can achieve instant tightening and lifting effect with moisturizing ingredients such as hyaluronic acid and glycerin.

Peptide Collaborative Anti Wrinkle Product: Combined with Acetyl Hexapeptide-8 (Argireline), a "dual neurotransmitter inhibition" full chain anti wrinkle system is constructed to achieve a synergistic anti wrinkle effect of 1+1>2.

4、 Formula recommendations and safety compliance

Gold synergy combination:

Compound with Acetyl Hexapeptide-8 (Argireline) (Best Partner): Both belong to the category of "botulinum toxin" peptides, but have different targets of action - Pentapeptide-3 targets postsynaptic membrane nAChRs (competitive antagonism), while Argireline targets presynaptic membrane SNAP-25 (inhibition of vesicle release), working together to block neuromuscular signal transmission and achieve a more comprehensive anti wrinkle effect. Clinical evidence has shown that the combination of the two has a significant synergistic effect.

With SYN-AKE ® Compound of snake venom tripeptide: SYN-AKE ® Similarly targeting nAChRs but with different sequences, the two can form a multi-target synergistic blockade.

Compound with hyaluronic acid: Pentapeptide-3 is responsible for relaxing muscles and reducing dynamic lines, while hyaluronic acid provides instant moisturizing and filling, both internally and externally.

Compound with nicotinamide: Pentapeptide-3 is responsible for anti wrinkle and firming, while nicotinamide is responsible for brightening skin tone, improving barriers, and comprehensively enhancing skin quality.

Compatibility and process suggestions: Pentapeptide-3 has good water solubility and is compatible with most water-based formulations. It is recommended to add it in the post formulation stage under low temperature conditions, with a pH range of 5-7, to preserve its biological activity to the greatest extent possible. Powder state -20 ℃ frozen storage, avoid repeated freezing and thawing after solution preparation.

Safety compliance: Pentapeptide-3 is a pure synthetic pentapeptide, not of animal origin, suitable for vegan (Vegan friendly) standards. Good water solubility, oil-free and wax free, with a acne rating of 0/5, suitable for all skin types including sensitive and acne prone skin. It does not increase photosensitivity and can be used during the day. High safety, minimal side effects, with only occasional reports of mild redness or stinging.

5、 Application Fields and Market Supply

Pentapeptide-3, as a classic synthetic peptide material for botulinum toxin, is widely used in the anti-aging skincare market.

Product positioning: Pentapeptide-3 is a potent anti wrinkle peptide that serves as a safe and gentle topical alternative to botulinum toxin injection. It instantly reduces expression lines (such as eyebrow wrinkles, smile lines, crow's feet, etc.) by relaxing facial muscles.

Application of international brands: Pentapeptide-3 is widely used in high-end skin care products focusing on the concepts of "botulinum toxin like" and "smearing anti wrinkle", including anti wrinkle essence, firming face cream, eye mask, facial mask and other product forms.

Market prospects: Pentapeptide-3, as one of the earliest "botulinum toxin" peptides to enter the market, is closely related to Argireline and SYN-AKE ® Ranked as one of the three classic neurotransmitter inhibitory peptides. Its unique advantage lies in its synergistic effect with Argireline, which has been clinically proven and plays an irreplaceable role in peptide based anti wrinkle formulations.