E-6837
E-6837 is a selective and orally active 5-HT6 receptor ligand. E-6837 demonstrates partial agonism at a presumably silent rat 5-HT6 receptor and full agonism at a constitutively active human 5-HT6 receptor by monitoring the cAMP signaling pathway. E-6837 induces hypophagia, reduces fat mass and body weight, and improves glycemic control. E-6837 can be used for the research of obesity.
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- CAS. Nr.: 528859-61-2
- Formel: C22H22ClN3O2S
- Molecular Weight:427.95
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Human 5-HT6 Receptor 9.13 (pKi) |
Rat 5-HT6 Receptor 8.37 (pIC50) |
Rat 5-HT6 Receptor 9.19 (pEC50) |
Human 5-HT6 Receptor 9.53 (pEC50) |
E-6837 binds selectively and with high affinity (pKi = 9.13 ± 0.17) to the recombinant human 5-HT6 receptor in HEK-293 membrane preparations[1].
E-6837 acts as a potent partial agonist (Emax = 67 ± 4%, pEC50 = 9.19 ± 0.11) and partial antagonist (Imax = 41 ± 3%, pIC50 = 8.37 ± 0.09) at the presumably silent rat 5-HT6 receptor stably expressed in HEK-293F cells[1].
E-6837 acts as a potent, nearly full agonist (Emax = 96 ± 4%, pEC50 = 9.53 ± 0.09) at the constitutively active human 5-HT6 receptor stably expressed in HEK-293F cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
E-6837 (60 mg/kg; p.o.; single dose) does not induce conditioned taste aversion or kaolin consumption in male Sprague-Dawley rats, indicating no emetic or aversive effects at these doses[1].
E-6837 (30 mg/kg; p.o.; twice daily; 28 days) induces a maximal 15.7% body weight loss in diet-induced obese female 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:Sprague-Dawley rats (male, 190 g at study start)[1]
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Dosage:5 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Reduced food intake transiently, with onset of suppression ~2 hours into the nightly feeding session, lasting ~6 hours (30 mg/kg dose).
Had no effect on food intake (5 mg/kg dose).
Did not alter locomotor activity (both doses) both.
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Animal Model:Sprague-Dawley rats (male, 6 weeks old, ~190 g at study start)[1]
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Dosage:60 mg/kg
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Administration:p.o.; single dose
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Result:Did not elicit conditioned taste aversion, with a saccharin preference ratio of 77.0 ± 10.7% (72-84 h) similar to vehicle (up to 60 mg/kg dose).
Had no effect on kaolin consumption at tested doses.
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Animal Model:Wistar rats (female, 250-300 g at study start, diet-induced obese via 12-week high-calorie cafeteria diet)[1]
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Dosage:30 mg/kg
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Administration:p.o.; twice daily; 28 days
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Result:Induced a maximal body weight loss of -15.7% over 28-day treatment period, with sustained weight loss for 3 weeks.
Reduced fat mass by 31.7%, with no significant changes in water, protein, or ash content.
Reduced plasma leptin levels by 49.6% (from 166 ± 19 ng/mL to 83 ± 19 ng/mL).
Improved glycemic control, with a significant reduction in plasma glucose excursion during glucose tolerance test and a trend toward reduced plasma insulin levels.
Resulted in transient rebound hyperphagia after treatment withdrawal, but body weight remained -6.6% lower than vehicle controls on day 71, with no profound rebound weight gain.
Decreased cumulative food intake by 31.7% during treatment period, with preferential reduction in chocolate intake.
Chemical Information
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CAS. Nr. 528859-61-2
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Molecular Weight 427.95
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Formel C22H22ClN3O2S
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SMILES
O=S(=O)(NC=1C=CC=2NC=C(C2C1)CCN(C)C)C=3C=CC=4C(Cl)=CC=CC4C3
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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