2. Neuronal Signaling Vitamin D Related/Nuclear Receptor
  3. Serotonin Transporter Estrogen Receptor/ERR
  4. 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.

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

SERT-IN-4

SERT-IN-4 Chemical Structure

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SERT-IN-4 Related Antibodies

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Description

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[1].

IC50 & Target[1]

ERα

3.66 nM (EC50)

In Vitro

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.

SERT-IN-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Significantly increased the viability of PC12 cells damaged by Corticosterone compared to the Corticosterone-only model group.
Parmacokinetics
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
In Vivo

SERT-IN-4 (Compound I11) (5-10 mg/kg; p.o.; daily; 14 days) dose-dependently reverses chronic unpredictable mild stress (CUMS)-induced depressive-like behaviors in male C57BL/6 mice[1].
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.

Animal Model: C57BL/6 (6-week-old male, 18−21 g, CUMS-induced)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 14 days
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.
Animal Model: C57BL/6 (6-week-old male, 18−21 g, CSDS-induced)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 14 days
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.
Molecular Weight

601.26

Formula

C38H49ClN2O2
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
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
References
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SERT-IN-4 Related Classifications

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Help & FAQs
  • 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.

Keywords:

SERT-IN-4Serotonin TransporterEstrogen Receptor/ERR5-HTTSERTSLC6A4p-CREBmajor depressive disorderC57BL/6 micehippocampal serotoninhuman SERTPC12 cellsERαBDNFhuman ERβHEK293T cellsInhibitorinhibitorinhibit

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