| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g | |||
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| Targets |
The primary target of α-Arbutin is tyrosinase, the key enzyme in melanin synthesis. It acts as a selective inhibitor, binding to tyrosinase and reducing its activity. By inhibiting tyrosinase, α-Arbutin decreases melanin production in melanocytes. This mechanism makes it highly effective in reducing hyperpigmentation, age spots, and uneven skin tone. It is commonly used in serums, creams, and lotions aimed at skin lightening and complexion improvement.
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| ln Vitro |
In vitro, α-Arbutin acts as a tyrosinase inhibitor. It suppresses the enzymes that stimulate melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases. α-Arbutin (30 mM) reduces postprandial plasma glucose levels in mice. It has also been used in the synthesis of α-glucosidase inhibitors.
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| ln Vivo |
In vivo, α-Arbutin (30 mM) reduces postprandial plasma glucose levels in mice. It is widely used in cosmetics as a depigmenting agent. The compound's skin-lightening effects have been demonstrated in various studies. It is commonly used in serums, creams, and lotions aimed at skin lightening and complexion improvement.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for α-Arbutin involve measuring its inhibition of tyrosinase activity. Tyrosinase enzyme is incubated with a substrate such as L-DOPA or tyrosine in the presence of varying concentrations of α-Arbutin. The production of melanin or dopachrome is measured spectrophotometrically. The IC50 for tyrosinase inhibition is determined from the inhibition curve. These assays confirm the compound's mechanism as a tyrosinase inhibitor.
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| Cell Assay |
In vitro cell-based assays for α-Arbutin are performed using melanocyte cell lines. Cells are treated with varying concentrations of α-Arbutin, and melanin production is measured. Cell viability is assessed to ensure that the compound does not cause cytotoxicity. The inhibition of tyrosinase activity and melanin synthesis is quantified. These assays confirm the compound's skin-lightening effects at the cellular level.
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| Animal Protocol |
In vivo animal experiments for α-Arbutin are conducted using mouse models. α-Arbutin (30 mM) is administered to mice, and postprandial plasma glucose levels are measured. The compound's effects on melanin production can be studied in animal models of hyperpigmentation. However, specific detailed protocols for in vivo melanin studies are limited in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of α-Arbutin indicate that it has a molecular weight of 272.25 and a molecular formula of C12H16O7. It is a glycosylated hydroquinone derivative. The compound is typically stored at -20°C. It is soluble in water and other polar solvents. Its absorption, distribution, metabolism, and excretion are characteristic of glycosylated compounds, with hydrolysis to hydroquinone being a potential metabolic pathway.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for α-Arbutin indicate that it is generally safe for use in cosmetic products. Compared to its β-isomer, α-Arbutin offers lower irritation potential. The compound is well-tolerated when applied topically. However, as a hydroquinone derivative, it should be used with caution, and long-term safety studies are ongoing. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
α-Arbutin is a glycoside. It has been reported that α-arbutin is found in Rhodiola rosea, Rhodiola rosea 'Aureomarginata', and other organisms with relevant data. See also: ... (See more...)
Other information: α-Arbutin is a popular and effective skin whitening agent. It is also known as 4-Hydroxyphenyl α-D-glucopyranoside. The compound is widely used in cosmetics as a depigmenting agent. It acts as a tyrosinase inhibitor in melanocytes. Its CAS number is 84380-01-8. |
| Molecular Formula |
C12H16O7
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|---|---|
| Molecular Weight |
272.253
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| Exact Mass |
272.089
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| CAS # |
84380-01-8
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| PubChem CID |
158637
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
561.6±50.0 °C at 760 mmHg
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| Melting Point |
195-196ºC
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| Flash Point |
293.4±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.650
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| LogP |
-1.35
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
279
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC(=CC=C1O)O[C@@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O
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| InChi Key |
BJRNKVDFDLYUGJ-ZIQFBCGOSA-N
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| InChi Code |
InChI=1S/C12H16O7/c13-5-8-9(15)10(16)11(17)12(19-8)18-7-3-1-6(14)2-4-7/h1-4,8-17H,5H2/t8-,9-,10+,11-,12+/m1/s1
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| Chemical Name |
(2R,3S,4S,5R,6R)-2-(hydroxymethyl)-6-(4-hydroxyphenoxy)oxane-3,4,5-triol
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| Synonyms |
4-Hydroxyphenyl α-D-Glucopyranoside α-Arbutin
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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 |
| 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) |
H2O : ~125 mg/mL (~459.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (183.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6731 mL | 18.3655 mL | 36.7309 mL | |
| 5 mM | 0.7346 mL | 3.6731 mL | 7.3462 mL | |
| 10 mM | 0.3673 mL | 1.8365 mL | 3.6731 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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