5-HT6R/FAAH modulator 2 

5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pK_i 7.24, human FAAH pIC₅₀ 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease^[1].

5-HT6R/FAAH modulator 2 (Compound 4c) potently binds to and antagonizes human 5-HT₆R with a pK_i of 7.24 and pKb of 7.00, while moderately inhibiting human recombinant FAAH with a pIC₅₀ of 5.47, and exhibits low affinity for off-target monoaminergic receptors^[1].
5-HT₆R/FAAH modulator 2 shows moderate metabolic stability in rat liver microsomes, with a half-life of 44 min and intrinsic clearance of 15.8 μL min⁻¹·mg⁻¹, and is metabolized primarily via sulfur oxidation^[1].
5-HT₆R/FAAH modulator 2 (0.8-20 μM; 1 h pre-incubation, 24 h co-incubation with okadaic acid) significantly preserves cell membrane integrity in okadaic acid-treated SH-SY5Y neuroblastoma cells^[1].
5-HT₆R/FAAH modulator 2 (10 μM) does not modulate β-amyloid aggregation^[1].
5-HT₆R/FAAH modulator 2 (10 μM; 1 h pre-incubation, 24 h co-incubation with glutamate) significantly protects HT-22 hippocampal neuronal cells from glutamate-induced toxicity, preserving membrane integrity and partially reducing caspase-3/7 activity^[1].

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

510.65

C₂₆H₃₄N₆O₃S

COC1=C(C(OC)=C(C=C1)CN2CCN(CC2)C3=NC(C(C)(SC4=CC=CC=C4)C)=NC(N)=N3)OC

Room temperature in continental US; may vary elsewhere.

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

• [1]. Czarnota-Łydka K, et al. New chalcogen-optimized 1, 3, 5-triazines as dual 5-HT6R/FAAH modulators: a versatile approach to neurodegenerative disorders[J]. European Journal of Medicinal Chemistry, 2026: 118966.