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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C38H49ClN2O2
- Molecular Weight:601.26
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
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. Further protocols information, click here.
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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.
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 (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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Molecular Weight 601.26
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SERT-IN-4 Related Classifications
HY-184011 Related Classifications
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