SERT/NET-IN-1
SERT/NET-IN-1 is a blood-brain barrier-permeable SERT and NET inhibitor, with an IC50 of 11.2 nM against human SERT and an IC50 of 32.0 nM against human NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET-IN-1 can be used in studies related to premature ejaculation.
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- Fòrmula: C16H20N2OS
- Peso molecular:288.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
SERT/NET-IN-1 (compound 7) (1 μM; 0, 5, 15, 30, 60 min) exhibits excellent metabolic stability in human, mouse, rat, dog and monkey liver microsomes. The proportion of remaining parent compound ranges from 86.1% (rat) to 103% (dog) after 60 min, with 98.5% remaining in human liver microsomes[1].
SERT/NET-IN-1 (100 μM; 48 h) shows no obvious cytotoxicity in either HEK293 or HepG2 cells, with an IC50 of >100 μM in both cell lines[1].
SERT/NET-IN-1 (100 μM; 48 h) exhibits almost no agonistic activity on μ-opioid receptors, with an EC50 > 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293, HepG2 cell
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Concentration:0-100 μM
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Incubation Time:48 h
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Result:Showed no obvious cytotoxicity in either HEK293 or HepG2 cells, with an IC50 of > 100 μM in both cell lines.
SERT/NET-IN-1 (20 mg/kg; i.p.; single administration, tested 15 min post-dose) significantly prolongs the ejaculation latency period (from 223.3 s to 713.2 s) and reduces the number of ejaculations within 20 min (from 2.25 to 1.125) in the 8-OH-DPAT-induced premature ejaculation model of male Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (10 weeks old, trained for 4 weeks to establish stable sexual behavior); premature ejaculation model induced by intraperitoneal injection of 0.4 mg/kg 8-OH-DPAT 1 h before testing[1]
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Dosage:10 mg/kg and 20 mg/kg
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Administration:intraperitoneal injection 15 min before testing
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Result:At 10 mg/kg, showed no significant effect on ejaculation latency or the number of ejaculations.
At 20 mg/kg, significantly increased ejaculation latency from 223.3 s (pre-dose) to 713.2 s (post-dose) (p=0.0281) and reduced the number of ejaculations in 20 min from 2.25 to 1.125 (p=0.0313).
Had no significant effect on mount latency, intromission latency, post-ejaculatory interval, or copulatory rate, indicating no impairment of sexual motivation or erectile function.
Chemical Information
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Peso molecular 288.41
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Fòrmula C16H20N2OS
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SMILES
CCC(N(C1CCNCC1)C2=C3C=CSC3=CC=C2)=O
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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/NET-IN-1 Related Classifications
HY-182244 Related Classifications
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