13-Hydroxyisobakuchiol
13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50 = 0.58 μM) and norepinephrine transporter (NET) (IC50 = 0.69 μM) than for the serotonin transporter (SERT) (IC50 = 312.02 μM). 13-Hydroxyisobakuchiol increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression.
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- CAS. Nr.: 178765-49-6
- Formel: C18H24O2
- Molecular Weight:272.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 0.58 μM (dopamine transporter)
IC50: 0.69 μM (norepinephrine transporter)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
>10 μM
Compound: 19
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Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
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[PMID: 25710081] |
| K562 | IC50 |
>10 μM
Compound: 19
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Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
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[PMID: 25710081] |
In Vitro
13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol) (10 μM, 20 min) inhibits dopamine (DA), norepinephrine (NE) and 5-HT uptake by respective Tr-CHO cells (D8, N1, or S6)[1].
13-Hydroxyisobakuchiol (0.03-10 μM, 20 min) inhibits DA and NE uptake by human neuroblastoma cell line SK-N-SH cells[1].
13-Hydroxyisobakuchiol (0.03-333 μM, 15 min) inhibits DA and NE uptake by synaptosomes from rat striatum or hippocampus[1].
13-Hydroxyisobakuchiol (1-500 μM, 4 h) dose-dependently prevents MPP+-induced cell toxicity in D8 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:D8 cells
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Concentration:1, 10, 100, 500 μM
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Incubation Time:4 h
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Result:Dose-dependently prevented MPP+-induced cell toxicity.
Exhibited pEC50 and Emax values for protection against D8 lesion of -0.34 and 82.31%, respectively.
In Vivo
13-Hydroxyisobakuchiol (5, 20, and 100 mg/kg, i.p. once) improves the decreased activity of Reserpinized mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (2 months old, 18-22g)[1]
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Dosage:4, 20, and 100 mg/kg
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Administration:i.p., once
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Result:Induced a dose-dependent increase in locomotor activity.
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Animal Model:Male C57BL/6 mice (2 months old, 18-22g) subcutaneously injected with 10 mg/kg Reserpine (HY-N0480)[1]
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Dosage:5, 20, and 100 mg/kg
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Administration:i.p., once
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Result:Markedly and dose-dependently increased horizontal movement in in Reserpine-pretreated mice.
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Animal Model:Male C57BL/6 mice (2 months old, 18-22g)[1]
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Dosage:10 and 100 mg/kg
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Administration:i.p., once
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Result:Showed no significant place preference response in the reward system.
Chemical Information
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CAS. Nr. 178765-49-6
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Molecular Weight 272.38
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Formel C18H24O2
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SMILES
OC1=CC=C(/C=C/[C@](C)(C=C)C/C=C/C(C)(O)C)C=C1
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Synonyms
Delta3,2-Hydroxylbakuchiol
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
13-Hydroxyisobakuchiol Related Classifications
HY-N7506 Related Classifications
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