Hordenine hydrochloride
Based on 2 publication(s) in Google Scholar
Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine hydrochloride inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.
For research use only. We do not sell to patients.
- Purity : 99.82%
- CAS No.: 6027-23-2
- Formula: C10H16ClNO
- Molecular Weight:201.70
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Hordenine hydrochloride
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Biological Activity
Description
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ERK1 |
ERK2 |
IL-6 |
IL-1β |
TNF-α |
iNOS |
COX-2 |
D3 Receptor 6.6 μM (EC50) |
D3 Receptor 6.9 μM (Ki) |
Alpha-2A adrenergic receptor 7.4 μM (EC50) |
Alpha-2A adrenergic receptor 11 μM (Ki) |
5-HT2A Receptor 3.1 μM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
5.546 μM
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Inhibition of cAMP production in HEK293T cells expressing DRD2 assessed by chemiluminescence intensity after 15 mins of incubation at room temperature.
Inhibition of cAMP production in HEK293T cells expressing DRD2 assessed by chemiluminescence intensity after 15 mins of incubation at room temperature.
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36883794 |
In Vitro
Hordenine (50-75 μg/mL; 1 h pre-treatment) hydrochloride inhibits the secretion of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β in LPS-stimulated RAW264.7 macrophages, downregulates the mRNA expression of pro-inflammatory mediators, and upregulates M2 macrophage markers, inhibits the activation of AKT, NF-κB, and MAPK signaling pathways, and reduces the protein expression of iNOS and COX-2[3].
Hordenine (75 μg/mL; 1 h pretreatment) hydrochloride inhibits LPS-induced nuclear translocation of p65 in RAW264.7 macrophages[3].
Hordenine (0.5-1.0 mg/mL; 24 h) hydrochloride reduces biofilm formation in Pseudomonas aeruginosa PAO1 by up to 31% at subinhibitory concentrations without affecting planktonic cell viability[4].
Hordenine (0.5-1.0 mg/mL; 24 h) hydrochloride significantly inhibits the production of QS-related virulence factors (protease, elastase, pyocyanin, rhamnolipid, alginate, and pyoverdine) in Pseudomonas aeruginosa PAO1 in a concentration-dependent manner[4].
Hordenine (0.5-1.0 mg/mL; 24 h) hydrochloride inhibits swimming and swarming motility of Pseudomonas aeruginosa PAO1 in a concentration-dependent manner[4].
Hordenine (1.0 mg/mL; 24 h) hydrochloride inhibits the expression of key QS-related genes (lasI, lasR, rhlI, rhlR) in Pseudomonas aeruginosa PAO1, with the most significant effect being a 60% downregulation of lasR[4].
Hordenine (100 μM; 0-8 h) hydrochloride activates the AMPK/Nrf2/HO-1 signaling cascade in EpH4-Ev cells[1].
Hordenine (0.5-100 μM; 1 h/5 days) hydrochloride inhibits melanin content in human epidermal melanocytes by downregulating the expression of MITF, tyrosinase, TRP-1, and TRP-2, and inhibiting CREB phosphorylation, reduces melanin levels in reconstructed epidermis, inhibits tyrosinase activity, and suppresses cAMP production[2].
Hordenine (12.5-200 μM; 48 h) hydrochloride promotes the proliferation of mouse primary dermal papilla cells in a dose-dependent manner[5].
Hordenine (25-50 μM; 10 consecutive days) hydrochloride significantly enhances the colony-forming ability of primary mouse dermal papilla cells at a concentration of 50 μM[5].
Hordenine (25-50 μM; 24 h) hydrochloride increases the proportion of proliferating (Ki67-positive) primary mouse dermal papilla cells, promotes nuclear translocation of β-catenin, elevates the gene expression of key DPC activity markers (ALP, Versican, and Wnt3a), activates the gene expression of the Wnt/β-catenin signaling pathway, and increases ALP protein expression[5].
Hordenine (2-50 μM; 24 h) hydrochloride dose-dependently activates DRD2 in live 293T-Tango-PB cells, with a maximum effective concentration of 50 μM[6].
Hordenine (0-90 μM; 15 min) hydrochloride inhibits cAMP production in HEK293T cells expressing DRD2, with an IC50 of 5.546 μM[6].
Hordenine (25-50 μM; 7 days) hydrochloride attenuates age-related α-synuclein accumulation in C. elegans strain NL5901 via a DRD2-dependent pathway[6].
Hordenine hydrochloride binds to multiple GPCRs with low micromolar affinity, exhibiting the highest affinity for the 5-HT2A receptor (Ki = 3.1 μM) and the D3 receptor (Ki = 6.9 μM)[7].
Hordenine hydrochloride binds to human SERT (Ki = 4.0 μM) with higher affinity than to human DAT (Ki = 30 μM)[7].
Hordenine hydrochloride acts as a potent partial agonist at D3R (EC50 = 6.6 μM; Emax = 70%), a weak partial agonist at α1A-AR (EC50 = 38 μM; Emax = 23%), and a neutral antagonist at 5-HT2A R (Emax < 5%)[7].
Hordenine hydrochloride is a full agonist of the α2A-adrenergic receptor (EC50 = 7.4 μM; Emax = 109%)[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EpH4-Ev mouse mammary epithelial cells
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Concentration:25, 50, 100, 200 μM
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Incubation Time:2 h pretreatment; 24 h LPS stimulation
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Result:Exerted a notable impact on cell viability at 200 μM.
Showed no cytotoxic effect at 25, 50, and 100 μM.
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Cell Line:EpH4-Ev mouse mammary epithelial cells
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Concentration:25, 50, 100 μM
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Incubation Time:2 h pretreatment; 24 h LPS stimulation
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Result:Suppressed the LPS-induced increase in mRNA levels of TNF-α, IL-1β, and IL-6.
Further increased the level of IL-10.
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Cell Line:EpH4-Ev mouse mammary epithelial cells
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Concentration:25, 50, 100 μM
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Incubation Time:2 h pretreatment; 24 h LPS stimulation
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Result:Alleviated the LPS-triggered elevation of iNOS and COX-2 expression.\nDose-dependently reduced the expression of TLR4 and phosphorylated expression of p65 and IκBα.
Alleviated the phosphorylation levels of p38, JNK, and ERK.
Alleviated p65 nuclear translocation.
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Cell Line:EpH4-Ev mouse mammary epithelial cells
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Concentration:100 μM
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Incubation Time:0, 1, 2, 4, 8 h
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Result:Enhanced activation of the AMPK/Nrf2/HO-1 pathway after 2-4 h pretreatment.
Promoted Nrf2 translocation into the nucleus.
AMPK inhibitor compound C inhibited AMPK phosphorylation, Nrf2 upregulation, and HO-1 expression.
Nrf2 inhibitor retinoic acid inhibited Nrf2 activation, HO-1 expression, the decrease in MDA content, and the increase in CAT activity and GSH/GSSG ratio.
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Cell Line:human epidermal melanocytes (Cascade Biologics)
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Concentration:0.5, 5, 50, 100 μM
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Incubation Time:1 h
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Result:Inhibited cAMP production in a concentration-dependent manner.
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Cell Line:human epidermal melanocytes (Cascade Biologics)
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Concentration:0.5, 5, 50, 100 μM
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Incubation Time:1 h and 5 days
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Result:Suppressed CREB phosphorylation.
Decreased MITF expression significantly in a concentration-dependent manner.
Inhibited the production of tyrosinase, TRP-1, and TRP-2.
At 100 μM, tyrosinase/β-actin, TRP-1/β-actin, and TRP-2/β-actin ratios were reduced to approximately 0.35, 0.4, and 0.35, respectively.
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Cell Line:LPS-stimulated RAW264.7 macrophages
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Concentration:50, 75 μg/mL
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Incubation Time:1 h (pre-treatment); 12 h (LPS stimulation)
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Result:Suppressed the LPS-induced increases in TNF-α, IL-6, and IL-1β protein levels.
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Cell Line:LPS-stimulated RAW264.7 macrophages
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Concentration:50, 75 μg/mL
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Incubation Time:1 h (pre-treatment); LPS stimulation
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Result:Reduced the LPS-induced mRNA expression of IL-6, TNF-α, iNOS, and COX-2.
Promoted the expression of M2 macrophage marker genes Arg-1, Ym-1, and CD206.
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Cell Line:LPS-stimulated RAW264.7 macrophages
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Concentration:50, 75 μg/mL
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Incubation Time:1 h (pre-treatment); 1 h (LPS stimulation)
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Result:Reduced the LPS-induced increases in iNOS and COX-2 protein levels.
Alleviated the increased phosphorylation levels of AKT, p65, IκB, p38, ERK1/2, and JNK induced by LPS.
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Cell Line:LPS-stimulated RAW264.7 macrophages
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Concentration:75 μg/mL
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Incubation Time:1 h (pre-treatment); 12 h (LPS stimulation)
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Result:Inhibited the LPS-induced nuclear translocation of p65.
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Cell Line:primary mouse dermal papilla cells (DPCs)
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Concentration:0, 12.5, 25, 50, 100, 200 μM
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Incubation Time:48 h
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Result:Showed safety at 200 μM.
Significantly increased cell proliferation at 12.5, 25, 50, and 100 μM, with the highest increase observed at 50 μM.
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Cell Line:primary mouse dermal papilla cells (DPCs)
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Concentration:0, 25, 50 μM
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Incubation Time:24 h
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Result:Increased the percentage of Ki67-positive DPCs in a dose-dependent manner, with counts rising from 10 (control) to 28 (25 μM) and 39 (50 μM) per 100 cells.\nGreatly promoted the nuclear entrance of β-catenin in DPCs compared with the controls.
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Cell Line:primary mouse dermal papilla cells (DPCs)
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Concentration:0, 25, 50 μM
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Incubation Time:24 h
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Result:Markedly upregulated the mRNA levels of ALP, Versican, and Wnt3a in a dose-dependent manner.\nMarkedly upregulated the mRNA expression of β-catenin, Lef-1, Axin2, and Cyclin D1 in a dose-dependent manner.
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Cell Line:primary mouse dermal papilla cells (DPCs)
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Concentration:0, 25, 50 μM
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Incubation Time:24 h
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Result:Markedly upregulated the protein levels of ALP in a dose-dependent manner.\nSignificantly increased the protein levels of p-GSK3β, β-catenin, Lef-1, Axin2, and Cyclin D1.
In Vivo
Hordenine (10-15 mg/kg; i.p.; single administration; 1 h before LPS modeling) hydrochloride attenuates LPS-induced acute lung injury in mice in a dose-dependent manner by inhibiting inflammation and the production of inflammatory cytokines[3].
Hordenine (30-100 mg/kg/day; p.o.; daily; 12 days) hydrochloride significantly ameliorates MPTP (HY-15608)-induced motor deficits and gait abnormalities in mice, rescues 44.4% of the climbing time, and restores multiple gait parameters[6].
Hordenine (100 mg/kg; p.o.; daily; 22 days) hydrochloride significantly ameliorates motor deficits in the 6-OHDA-induced hemiparkinsonian mouse model, reducing climbing time by 22.2% and traversal time by 34.2%[6].
Hordenine (50 mg/kg; i.p.; once daily; for 4 consecutive days) hydrochloride attenuates persistent alcohol intake in mice and prophylactically reduces relapse behavior after withdrawal[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (25-30 g, 7-8 weeks old, female)[1]
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Dosage:50 mg/kg/day
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Administration:p.o.; daily; 14 days
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Result:Reduced histopathological scores in mammary tissue from 3.75 to 1.75.
Attenuated the LPS-induced increase in MPO activity.
Reduced levels of pro-inflammatory mediators (IL-6, TNF-α, IL-1β, COX-2, iNOS) while elevating the anti-inflammatory cytokine IL-10.
Restored the integrity of the blood-milk barrier by upregulating the expression of tight junction proteins ZO-1, occludin, and claudin-3.
Inhibited the LPS-induced phosphorylation of key proteins in the TLR4-MAPK/NF-κB pathway while activating the AMPK/Nrf2/HO-1 antioxidative pathway.
Mitigated the LPS-induced increase in MDA content and restored decreased CAT activity, GSH/GSSG ratio, and SOD activity.
Altered the composition of intestinal microbiota, increasing the abundance of Lactobacillaceae, S24-7, and Prevotellaceae at the family level and Lactobacillus at the genus level, while decreasing Bacteroidaceae, Desulfovibrionaceae, Lachnospiraceae, and Ruminococcaceae at the family level and Bacteroides, Desulfovibrio, Oscillospira, and Blautia at the genus level.\nReduced histopathological damage in recipient mice.
Reduced MPO activity, IL-1β, IL-6, TNF-α, iNOS, and COX-2 levels, and elevated IL-10 levels.
Enhanced expression of tight junction proteins ZO-1 (fold change ~2.0), occludin (fold change ~1.8), and claudin-3 (fold change ~4.0) compared to the FN group.
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Animal Model:BALB/c mice (Male, 6-8 weeks old, LPS-induced)[3]
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Dosage:10, 15 mg/kg
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Administration:i.p.; single dose; 1 h before LPS modeling
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Result:Reduced lung histopathological injury score in a dose-dependent manner, with the 15 mg/kg dose showing greater alleviation than the 10 mg/kg dose.
Decreased the lung wet-dry (W/D) weight ratio.
Reduced mRNA expression levels of Il6, Il1β, Tnfa, iNOS, Cox2, and Mpo in lung tissues.
Reduced protein secretion of IL-6, IL-1β, and TNF-α in bronchoalveolar lavage fluid (BALF).
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Animal Model:C57BL/6 (female, 7-week-old)[5]
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Dosage:1 mM; 2 mM
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Administration:topical application; daily; 25 days
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Result:Accelerated anagen entry and hair regrowth.
Significantly increased the rate of hair regeneration at both 1 mmol/L and 2 mmol/L.
Markedly promoted hair follicles to enter a state of active growth at day 6.
Markedly increased the protein levels of β-catenin, p-GSK3β, and Axin2, and greatly increased the expression of downstream target genes Lef-1 and Cyclin D1 at both mRNA and protein levels.
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Animal Model:C57BL/6 (male, 12-week-old, 20-25 g, MPTP-induced)[6]
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Dosage:30, 100 mg/kg/day
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Administration:p.o.; daily; 12 days
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Result:Reduced turning and climbing time in the pole test, rescuing 44.4% of climbing time.
Improved locomotor speed, step size, and preserved shorter run duration in Catwalk gait analysis.
Rescued shortened bilateral print positions and recovered stride length of four limbs.
Presented similar or better effect than PPX on swing speed and relieved prolonged standing time and step cycle time.
Increased TH-immunopositive fiber fluorescence intensity in the striatum but did not change TH-immunopositive cells in the SNpc.
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Animal Model:C57BL/6 (male, 12-week-old, 20-25 g, 6-OHDA-induced)[6]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 22 days
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Result:Reduced climbing time by 22.2% in the pole test compared to the 6-OHDA-lesioned group.
Spent 34.2% less time to cross the beam in the balance beam test.
Regained almost 30% locomotion activity compared to the 6-OHDA group.
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Animal Model:C57BL/6 J mice (Male, 8 weeks old, 26 g)[7]
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Dosage:50 mg/kg
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Administration:i.p.; once a day; 4 days
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Result:Reduced ongoing alcohol consumption on the first treatment day and the second day after treatment, with a significant decrease in the 6-day average alcohol consumption.
Decreased the 6-day average alcohol preference and total intake.
Reduced alcohol consumption on the first, third, and fourth days of reinstatement, with a significant decline in the 4-day average consumption and preference during withdrawal.
Had no effect on alcohol consumption during relapse, but significantly decreased alcohol preference on the third reinstatement day and in the 4-day average analysis.
- RNA extraction experimental
- Somatic Cell Culture
- Phagocytosis Functional Assay
- Cytoplasmic-Nuclear Fractionated Protein Extraction
- Transepithelial/transendothelial electrical resistance assay
- Inhalation Toxicity Study
- MTT Cell Proliferation Assay
- Western Blot
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- LPS-Induced Endotoxemia/Systemic Inflammation
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Human pluripotent stem cell midbrain dopaminergic neuron differentiation
- Primary monocyte-to-macrophage differentiation
- Protocol for Kinase activity and phosphorylation assays
Chemical Information
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CAS No. 6027-23-2
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Appearance Solid
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Molecular Weight 201.70
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Formula C10H16ClNO
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Color White to off-white
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SMILES
OC1=CC=C(CCN(C)C)C=C1.[H]Cl
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Synonyms
Ordenina hydrochloride; Peyocactine hydrochloride
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Agric Food Chem
Chemoproteomic Profiling of Cobalamin-Independent Methionine Synthases in Plants with a Covalent Probe. [Abstract]2020 Jul 29;68(30):8050-8056. PMID: 32618189
Solvent & Solubility
In Vitro:
DMSO : 12.5 mg/mL (61.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (312 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[2]. Kim SC, et al. Hordenine, a single compound produced during barley germination, inhibits melanogenesis in human melanocytes. Food chemistry. 2013 Nov 01;141(1):174-81. [Content Brief]
[6]. Li H, et al. Hordenine improves Parkinsonian-like motor deficits in mice and nematodes by activating dopamine D2 receptor-mediated signaling. Phytotherapy research : PTR. 2023 Aug;37(8):3296-3308. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.9579 mL | 24.7893 mL | 49.5786 mL | 123.9465 mL |
| 5 mM | 0.9916 mL | 4.9579 mL | 9.9157 mL | 24.7893 mL | |
| 10 mM | 0.4958 mL | 2.4789 mL | 4.9579 mL | 12.3946 mL | |
| 15 mM | 0.3305 mL | 1.6526 mL | 3.3052 mL | 8.2631 mL | |
| 20 mM | 0.2479 mL | 1.2395 mL | 2.4789 mL | 6.1973 mL | |
| 25 mM | 0.1983 mL | 0.9916 mL | 1.9831 mL | 4.9579 mL | |
| 30 mM | 0.1653 mL | 0.8263 mL | 1.6526 mL | 4.1315 mL | |
| 40 mM | 0.1239 mL | 0.6197 mL | 1.2395 mL | 3.0987 mL | |
| 50 mM | 0.0992 mL | 0.4958 mL | 0.9916 mL | 2.4789 mL | |
| 60 mM | 0.0826 mL | 0.4132 mL | 0.8263 mL | 2.0658 mL |
Hordenine hydrochloride Related Classifications
HY-N0113B Related Classifications
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Keywords
- Hordenine
- 6027-23-2
- Ordenina
- Peyocactine
- Bacterial
- p38 MAPK
- JNK
- ERK
- Akt
- Interleukin Related
- TNF Receptor
- NO Synthase
- COX
- Reactive Oxygen Species (ROS)
- Microphthalmia Associated Transcription Factor (MITF)
- Wnt
- β-catenin
- Dopamine Receptor
- Adrenergic Receptor
- 5-HT Receptor
- Serotonin Transporter
- Dopamine Transporter
- α-synuclein
- TRP-1
- tyrosinase
- MITF
- cAMP
- Nrf2
- HO-1
- TLR4
- NF-κB
- AMPK
- MAPK
- Inhibitor
- inhibitor
- inhibit