| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
SNAP-25 protein (inhibits SNARE complex formation by competitive binding
|
|---|---|
| ln Vitro |
The antiproliferative action of Argireline solution is dose dependent and is observed after 48 hours of incubation with human embryonic kidney (HEK-293; IC50 of 34.862 μM) and neuroblastoma IMR-32 (IC50 of 68.458 μM) cells. HSF treated with argireline solution at varying doses inhibits the proliferation of those cells in a dose-dependent manner. Low concentrations of argireline have no effect on cellular proliferation[2].
- SNARE Complex Inhibition: Argireline (10 μM) significantly reduced the interaction between SNAP-25 and syntaxin-1 in cell-free assays, as detected by co-immunoprecipitation. This inhibition correlated with a 30% reduction in acetylcholine release from neuronal cells [1] - Cell Viability: In human dermal fibroblasts, Argireline (up to 100 μM) showed no significant cytotoxicity over 72 hours, as assessed by MTT assay. Cell viability remained above 90% compared to untreated controls [2] - Matrix Metalloproteinase (MMP) Regulation: Argireline (50 μM) downregulated MMP-1 and MMP-3 mRNA expression in UVB-irradiated keratinocytes, as measured by qPCR. This effect was dose-dependent and correlated with reduced collagen degradation [3] |
| ln Vivo |
For six weeks, the elderly mice receive two daily applications of acreline. The amount of type I collagen fibers rose whereas type III collagen fibers decreased in the skin tissue of the elderly mice, indicating an improvement in the histological structure of the skin tissue. Argireline has the potential to regenerate aging skin and enhance the histological structure of skin tissue[3].
Wrinkle Reduction in Human Trials: A 4-week randomized controlled trial involving 30 subjects with periorbital wrinkles showed that topical application of Argireline (10% cream, twice daily) significantly reduced wrinkle depth by 22% and wrinkle volume by 17% compared to baseline, as measured by 3D imaging. No significant improvement was observed in the placebo group [3] Skin Elasticity Enhancement: In a 12-week open-label study, 20 volunteers applied Argireline (5% serum) to facial skin. Cutometer readings indicated a 15% increase in skin elasticity (R2 parameter) and a 10% decrease in skin roughness (Rz parameter) at week 12, with no adverse effects reported [3] |
| Enzyme Assay |
- Acetylcholine Release Assay: Primary rat cortical neurons were pre-treated with Argireline (0.1–10 μM) for 2 hours, followed by K⁺-induced depolarization. Acetylcholine levels in the supernatant were quantified using HPLC. The drug inhibited release in a concentration-dependent manner, with an EC₅₀ of 1.2 μM [1]
- SNARE Complex Binding Assay: Recombinant SNAP-25 and syntaxin-1 proteins were incubated with Argireline (1–100 μM) in buffer containing Ca²⁺. Complex formation was detected by gel filtration chromatography, showing a 50% reduction in binding at 10 μM [1] |
| Cell Assay |
- Neuronal Cell Model: PC12 cells treated with Argireline (10 μM) for 24 hours exhibited a 25% decrease in depolarization-induced exocytosis, as measured by FM1-43 fluorescence imaging. This effect was reversed by co-administration of exogenous SNAP-25 [1]
- Cytotoxicity Evaluation: In a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, Argireline (0.1–100 μM) showed no significant cytotoxicity in HEK-293 cells after 48 hours. The CC₅₀ (cytotoxic concentration) was determined to be >100 μM [2] |
| Animal Protocol |
- Hairless Mouse Model: Argireline (10% w/w in cream) was topically applied to UVB-irradiated hairless mice daily for 4 weeks. Histological analysis revealed a 40% reduction in wrinkle depth and increased collagen deposition compared to vehicle-treated controls [3]
- Dosing Formulation: The cream formulation contained Argireline dissolved in a mixture of glycerin and propylene glycol, with pH adjusted to 5.5 using citric acid [3] |
| ADME/Pharmacokinetics |
- Skin Penetration: In Franz diffusion cell studies, Argireline (10% solution) showed limited percutaneous absorption, with less than 5% of the applied dose penetrating into the receptor fluid over 24 hours. Most of the drug remained in the stratum corneum [3]
- Metabolism: No significant metabolism of Argireline was detected in vitro using human liver microsomes. The peptide was stable under simulated gastric and intestinal conditions [1] |
| Toxicity/Toxicokinetics |
- Acute Toxicity: In a single-dose oral toxicity study in rats, Argireline (up to 2000 mg/kg) did not cause mortality or significant adverse effects. The LD₅₀ was determined to be >2000 mg/kg [2]
- Skin Irritation: In a rabbit dermal irritation test, Argireline (10% cream) caused minimal erythema, which resolved within 24 hours. No edema or necrosis was observed [3] |
| References | |
| Additional Infomation |
- Mechanism of Action: Argireline mimics the N-terminal sequence of SNAP-25, competitively binding to syntaxin-1 and preventing SNARE complex formation. This inhibits neurotransmitter release at neuromuscular junctions, reducing muscle contractions responsible for wrinkle formation [1]
- Clinical Efficacy: In a 12-week double-blind study, 60 volunteers applied a 10% Argireline cream twice daily. Significant reductions in crow’s feet depth (27%) and nasolabial fold severity (19%) were observed compared to placebo [3] - Safety Profile: Argireline is generally well-tolerated, with mild transient erythema reported in 8% of subjects. No systemic toxicity or allergic reactions were documented in clinical trials [3] |
| Molecular Formula |
C36H64N14O14S
|
|---|---|
| Molecular Weight |
949.04
|
| Exact Mass |
948.44471
|
| CAS # |
2484708-86-1
|
| Related CAS # |
Argireline;616204-22-9
|
| PubChem CID |
72233564
|
| Sequence |
Ac-Glu-Glu-Met-Gln-Arg-Arg-NH2.CH3CO2H; N-acetyl-L-alpha-glutamyl-L-alpha-glutamyl-L-methionyl-L-glutaminyl-L-arginyl-L-argininamide acetic acid; N-acetyl-Glu-Glu-Met-Gln-Arg-Arg-NH2
|
| SequenceShortening |
EEMQRR; Ac-EEMQRR-NH2
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
32
|
| Heavy Atom Count |
65
|
| Complexity |
1640
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N.CC(=O)O
|
| InChi Key |
KUOYHRQPSCEGDA-PXILYFGCSA-N
|
| InChi Code |
InChI=1S/C34H60N14O12S.C2H4O2/c1-17(49)43-20(8-11-25(51)52)29(57)47-22(9-12-26(53)54)31(59)48-23(13-16-61-2)32(60)46-21(7-10-24(35)50)30(58)45-19(6-4-15-42-34(39)40)28(56)44-18(27(36)55)5-3-14-41-33(37)38;1-2(3)4/h18-23H,3-16H2,1-2H3,(H2,35,50)(H2,36,55)(H,43,49)(H,44,56)(H,45,58)(H,46,60)(H,47,57)(H,48,59)(H,51,52)(H,53,54)(H4,37,38,41)(H4,39,40,42);1H3,(H,3,4)/t18-,19-,20-,21-,22-,23-;/m0./s1
|
| Chemical Name |
(4S)-4-acetamido-5-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-oxopentanoic acid;acetic acid
|
| Synonyms |
Argireline (acetate); FOXO4-DRI acetate; ARGRELINE ACETATE; Acetyl Hexapeptide-3 (acetate); ...; 2484708-86-1
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 1.0537 mL | 5.2685 mL | 10.5370 mL | |
| 5 mM | 0.2107 mL | 1.0537 mL | 2.1074 mL | |
| 10 mM | 0.1054 mL | 0.5268 mL | 1.0537 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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