| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
Hordenine (Ordenina; Peyocactine) is a naturally occuring phenylethylamine alkaloid found in plants with antibacterial and antibiotic properties. It inhibits the uptake of norepinephrine in mammals, working as a stimulant. It is produced in nature by several varieties of plants in the family Cactaceae and by some in Acacia. Recent study shows that hordenine may be an effective inhibitor of hyperpigmentation. it inhibits melanogenesis by suppressing cAMP production, which is involved in the expression of melanogenesis-related proteins
| Targets |
Tyrosinase (IC50 = 2.3 mM); Melanogenesis-related proteins (MITF, TRP-1, TRP-2) (Cellular IC50 for melanin inhibition = ~1 mM) [1]
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| ln Vitro |
Hordenine (N,N-dimethyl-4-hydroxyphenylethylamine) is a phenylethylamine alkaloid with antibacterial and antibiotic properties. It inhibits the uptake of norepinephrine in mammals, working as a stimulant. It is produced in nature by several varieties of plants in the family Cactaceae and by some in Acacia. Recent study shows that hordenine may be an effective inhibitor of hyperpigmentation. it inhibits melanogenesis by suppressing cAMP production, which is involved in the expression of melanogenesis-related proteins.
Hordenine (Ordenina; Peyocactine) potently inhibits melanogenesis in human epidermal melanocytes (HEMn-DP) without cytotoxicity. It suppressed tyrosinase activity (the key enzyme in melanin synthesis) in a dose-dependent manner, with an IC50 of 2.3 mM [1] - At concentrations of 0.5-2 mM, Hordenine (Ordenina; Peyocactine) reduced intracellular melanin content by ~28% (0.5 mM), ~45% (1 mM), and ~62% (2 mM) compared to the control group. It also inhibited extracellular melanin secretion by ~22% (0.5 mM), ~39% (1 mM), and ~58% (2 mM) [1] - The anti-melanogenic effect was associated with downregulating the expression of melanogenesis-related proteins and mRNA. It reduced MITF (microphthalmia-associated transcription factor) protein levels by ~35% (1 mM) and ~55% (2 mM), and decreased TRP-1 (tyrosinase-related protein 1) and TRP-2 expression by ~30% and ~28% (1 mM), respectively. Corresponding mRNA levels of MITF, TRP-1, and TRP-2 were also reduced by ~40%, ~32%, and ~29% at 1 mM [1] - No significant cytotoxicity was observed in HEMn-DP cells or normal human keratinocytes (HaCaT) at concentrations up to 5 mM, as confirmed by MTT assay [1] |
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| ln Vivo |
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| Enzyme Assay |
Tyrosinase activity assay: Purified mushroom tyrosinase was incubated with L-3,4-dihydroxyphenylalanine (L-DOPA, substrate) and different concentrations of Hordenine (Ordenina; Peyocactine) (0.5-5 mM) at 37°C for 60 minutes. The oxidation product of L-DOPA was measured spectrophotometrically at 475 nm, and tyrosinase inhibition rate was calculated to determine the IC50 value [1]
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| Cell Assay |
Melanin content assay: Human epidermal melanocytes (HEMn-DP) were seeded in 6-well plates and treated with Hordenine (Ordenina; Peyocactine) (0.5-2 mM) for 72 hours. Cells were lysed with lysis buffer, and melanin was solubilized in 1 M NaOH at 80°C for 1 hour. Melanin content was quantified by measuring absorbance at 405 nm and normalized to total protein concentration [1]
- Western blot and PCR assay: HEMn-DP cells were treated with Hordenine (Ordenina; Peyocactine) (0.5-2 mM) for 48 hours. Western blot was used to detect MITF, TRP-1, and TRP-2 protein expression; total RNA was extracted, and reverse transcription-PCR was performed to measure the mRNA levels of these melanogenesis-related genes [1] - Cell viability assay: HEMn-DP cells and HaCaT cells were seeded in 96-well plates and treated with Hordenine (Ordenina; Peyocactine) (0.5-5 mM) for 72 hours. MTT reagent was added, and the absorbance at 570 nm was measured to evaluate cell viability [1] |
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| Animal Protocol |
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| Toxicity/Toxicokinetics |
In vitro experiments showed that phycocactine at concentrations up to 5 mM had no cytotoxicity against HEMn-DP melanocytes and HaCaT keratinocytes [1].
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| References | |||
| Additional Infomation |
Holdenin is a phenylethylamine alkaloid. It is a metabolite in both humans and mice. Holdenin has been reported in Laurencia pinnatifida, Senegalia berlandieri, and other organisms with relevant data. See also: Holdenin hydrochloride (its active ingredient). Stem (part) of Calendula grandiflora.
Ordenina (Peyocactine) is a phenylethylamine alkaloid that is naturally produced during the germination of barley (Hordeum vulgare L.)[1] - Its anti-melanogenesis mechanism includes two key steps: direct inhibition of tyrosinase activity and downregulation of MITF-mediated signaling pathways, thereby reducing the expression of melanogenesis-related proteins (TRP-1, TRP-2)[1] - Due to its low cytotoxicity and strong melanin-inhibiting activity, it has potential application value in the development of whitening cosmetics or topical preparations[1] |
| Molecular Formula |
C10H15NO
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| Molecular Weight |
165.23
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| Exact Mass |
165.115
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| Elemental Analysis |
C, 72.69; H, 9.15; N, 8.48; O, 9.68
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| CAS # |
539-15-1
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| Related CAS # |
Hordenine-d6;1346598-66-0
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| PubChem CID |
68313
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
270.2±23.0 °C at 760 mmHg
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| Melting Point |
117.5 °C
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| Flash Point |
123.5±21.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.542
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
12
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| Complexity |
117
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
KUBCEEMXQZUPDQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15NO/c1-11(2)8-7-9-3-5-10(12)6-4-9/h3-6,12H,7-8H2,1-2H3
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| Chemical Name |
4-[2-(dimethylamino)ethyl]phenol
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| Synonyms |
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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 |
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| 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 : 33~250 mg/mL ( 199.72~1513.04 mM )
Ethanol : ~33 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (37.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (37.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (37.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 6.25 mg/mL (37.83 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.0522 mL | 30.2608 mL | 60.5217 mL | |
| 5 mM | 1.2104 mL | 6.0522 mL | 12.1043 mL | |
| 10 mM | 0.6052 mL | 3.0261 mL | 6.0522 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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