LuAF60097
LuAF60097 is a serotonin transporter (SERT) ligand. LuAF60097 binds to the extracellular vestibule (S2 site) of SERT with high affinity and to the central binding site (S1) with lower affinity, triggering conformational changes that exert combined competitive and non-competitive inhibitory effects on serotonin reuptake. LuAF60097 is applicable to research related to depression and anxiety disorders.
For research use only. We do not sell to patients.
- CAS No.: 2507890-46-0
- Formula: C32H32FN3O3
- Molecular Weight:525.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
LuAF60097 (30-70 min) acts as a high-affinity allosteric inhibitor of hSERT WT expressed in COS-7 cell membranes, with ~210-fold higher potency for inhibiting [3H]IMI dissociation (IC50 = 31 nM) compared to [3H]S-CIT dissociation (IC50 = 6500 nM)[1].
LuAF60097 (1 h) binds to the orthosteric S1 site of hSERT WT expressed in COS-7 cell membranes with an IC50 of 270 nM, and does not displace pre-bound [3H]IMI[1].
LuAF60097 (15-20 min) inhibits [3H]5-HT uptake in intact COS-7 cells expressing hSERT WT (IC50 = 207 nM) or hSERT F556R (IC50 = 260 nM) with similar potency[1].
LuAF60097 inhibits [3H]5-HT uptake in intact COS-7 cells expressing hSERT WT through a combined competitive (increased KM) and non-competitive (decreased VMAX) mechanism[1].
LuAF60097 (27 nM; 3 min) and Imipramine (HY-B1490A) (4 nM) act synergistically to inhibit [3H]5-HT uptake in intact COS-7 cells expressing hSERT WT, producing a significantly greater inhibitory effect than either compound alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LuAF60097 (1.9 µM; continuous local intracerebral perfusion) alone does not alter hippocampal 5-HT levels, but when combined with 0.36 µM Imipramine, it synergistically increases extracellular 5-HT levels in rat hippocampus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (male, 300-400 g)[1]
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Dosage:250 nM
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Administration:local intracerebral injection; single dose
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Result:Increased hippocampal extracellular 5-HT levels significantly starting 80 minutes post-injection, reaching a maximum of 602% of basal levels (saline control) at 120 minutes post-injection.
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Animal Model:Sprague Dawley (male, 300-400 g)[1]
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Dosage:1.9 µM (alone); 1.9 µM (in combination with 0.36 µM imipramine)
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Administration:continuous local intracerebral perfusion
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Result:Did not significantly alter hippocampal extracellular 5-HT levels relative to saline when administered alone.
When perfused in combination with 0.36 µM imipramine, increased extracellular 5-HT levels significantly starting 40 minutes post-perfusion, remained elevated for the duration of the 160-minute period, and showed a significantly higher area under the curve compared to either compound alone or saline.
Chemical Information
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CAS No. 2507890-46-0
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Molecular Weight 525.62
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Formula C32H32FN3O3
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SMILES
C(CCN1CCC(CC1)C=2C=C3C(=CC2)C=CC(=O)N3)[C@@]4(C=5C(CO4)=CC(C(N)=O)=CC5)C6=CC=C(F)C=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LuAF60097 Related Classifications
HY-187650 Related Classifications
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