SERT-IN-4
SERT-IN-4 is a brain-penetrant and orally active SERT inhibitor and ERβ agonist with human SERT IC50 of 16.92 nM and human ERβ EC50 of 3.66 nM. SERT-IN-4 inhibits SERT-mediated substrate transport, increases hippocampal serotonin levels, modulates p-CREB and BDNF expression.SERT-IN-4 reduces immobility in CUMS mice, improves social interaction and reduces inactivity in CSDS mice.SERT-IN-4 can be used for the research of major depressive disorder.
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- Fòrmula: C38H49ClN2O2
- Peso molecular:601.26
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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ERα 3.66 nM (EC50) |
SERT-IN-4 (Compound I11) forms specific, high-affinity interactions with both human SERT and human ERβ proteins, with structural features that enhance binding and ERβ selectivity[1].
SERT-IN-4 (0.1 μM; 24 h) significantly protects PC12 cells against Corticosterone (HY-B1618)-induced damage[1].
SERT-IN-4 (0.01-10 μM; 24 h) acts as a potent, selective ERβ agonist in HEK293T cells, with an ERβ EC50 of 3.66 nM[1].
SERT-IN-4 (0.1 nM-10 μM; 30 min) potently inhibits human SERT function in HEK293T cells, with an IC50 of 16.92 nM for hSERT-mediated APP+ uptake[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Significantly increased the viability of PC12 cells damaged by Corticosterone compared to the Corticosterone-only model group.
| Species | Dose | Route | Tmax (Plasma) | AUC0-∞ (Plasma) | T1/2 (Plasma) | Tmax (Brain) | Cmax (Brain) | AUC0-∞ (Brain) | T1/2 (Brain) |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 1.00 h | 4125.29 ng·h/mL | 6.04 h | 1.00 h | 323.55 ng/g | 3824.26 ng·h/mL | 12.11 h |
SERT-IN-4 (5-10 mg/kg; p.o.; daily; 14 days) dose-dependently reverses CSDS-induced depressive-like behaviors in male C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (6-week-old male, 18−21 g, CUMS-induced)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Increased total travel distance (p < 0.01) and average speed (p < 0.01) in OFT, reduced immobility time in FST (p < 0.0001), increased sucrose preference index (p < 0.01), reduced fecal output in OFT (p < 0.001), and improved alignment and reduced damage of hippocampal pyramidal and granule cells at 5 mg/kg dose compared to model group.
Increased total travel distance (p < 0.01) and average speed (p < 0.05) in OFT, reduced immobility time in FST (p < 0.0001) and TST (p < 0.0001), increased sucrose preference index (p < 0.01), reduced fecal output in OFT (p < 0.001) with the most pronounced reduction among treatment groups, and improved alignment and reduced damage of hippocampal pyramidal and granule cells at 10 mg/kg dose compared to model group.
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Animal Model:C57BL/6 (6-week-old male, 18−21 g, CSDS-induced)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Increased social interaction ratio in SIT (p < 0.001), reduced immobility time in FST (p < 0.05) and TST (p < 0.05), increased sucrose preference index (p < 0.0001), elevated hippocampal 5-HT levels (p < 0.0001), upregulated p-CREB (p < 0.05), BDNF (p < 0.05), and ERβ (p < 0.01) expression, and downregulated SERT expression (p < 0.001) at 5 mg/kg dose compared to model group.
Increased social interaction ratio in SIT (p < 0.0001), reduced immobility time in FST (p < 0.0001) and TST (p < 0.0001), increased sucrose preference index (p < 0.0001), elevated hippocampal 5-HT levels (p < 0.0001), upregulated p-CREB (p < 0.01), BDNF (p < 0.01), and ERβ (p < 0.001) expression, and downregulated SERT expression (p < 0.0001) at 10 mg/kg dose compared to model group.
Chemical Information
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Peso molecular 601.26
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Fòrmula C38H49ClN2O2
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SMILES
[H][C@@]12CCC3=C([C@]1(CC[C@]4([C@]2(CC[C@@H]4O)[H])C)[H])C=CC(OCCCCCCCN5CCC(C6=CNC7=CC(Cl)=CC=C76)=CC5)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SERT-IN-4 Related Classifications
HY-184011 Related Classifications
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