1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  2. 5-HT Receptor FAAH Apoptosis Reactive Oxygen Species (ROS)
  3. 5-HT6R/FAAH modulator 1

5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pKi of 6.33 (5-HT6) and a pIC50 valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC50 = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

For research use only. We do not sell to patients.

5-HT6R/FAAH modulator 1

5-HT6R/FAAH modulator 1 Chemical Structure

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Description

5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pKi of 6.33 (5-HT6) and a pIC50 valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC50 = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD)[1].

IC50 & Target[1]

5-HT6 Receptor

6.33 (pKi)

In Vitro

5-HT6R/FAAH modulator 1 (Compound 23) (0.3-30 μM, 72 h) inhibits HepG2 and SH-SY5Y cells growth[1].
5-HT6R/FAAH modulator 1 (10 μM, 17 h) increases cell viability and inhibits apoptosis and reduces ROS levels in Aβ1-42-treated HT-22 cells[1].
5-HT6R/FAAH modulator 1 (0.03-0.15 μM) shows potent antioxidant activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HepG2 and SH-SY5Y cells
Concentration: 0.3, 3 and 30 μM
Incubation Time: 72 h
Result: Inhibited the growth of HepG2 cells by 30 % at a concentration of 3 μM.
Inhibited cell proliferation by only 44 % at the highest concentration of 30 μM.
In Vivo

5-HT6R/FAAH modulator 1 (Compound 23) (0.3-1 mg/kg, i.p.) reverses memory impairment in MK-801-induced memory impairment rats models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MK-801-induced memory impairment rats models[1]
Dosage: 0.3 and 1 mg/kg
Administration: Intraperitoneally injection
Result: Reversed memory deficits at a dose of 1 mg/kg producing a bell-shape effect.
Molecular Weight

494.59

Formula

C26H34N6O4

SMILES

NC1=NC(COC2=CC(C)=CC=C2C)=NC(N3CCN(CC4=CC=C(OC)C(OC)=C4OC)CC3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
5-HT6R/FAAH modulator 1
Cat. No.:
HY-175816
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