5-HT2C agonist-13
5-HT2C agonist-13 is an orally active, selective and brain-penetrant 5-HT2C receptor agonist with human 5-HT2C receptor EC50 of 16 nM, Ki of 20 nM. 5-HT2C agonist-13 functionally activates 5-HT2C receptors, reduces food intake, reduces body weight gain, and exhibits effects reversible by a selective 5-HT2C antagonist. 5-HT2C agonist-13 can be used for the research of obesity.
For research use only. We do not sell to patients.
- CAS No.: 850033-84-0
- Formula: C14H15F3N2O
- Molecular Weight:284.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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Human 5-HT2C Receptor 16 nM (EC50) |
Human 5-HT2C Receptor 20 nM (Ki) |
5-HT2A Receptor 4926 nM (EC50) |
5-HT2A Receptor 153 nM (Ki) |
5-HT2B Receptor 1170 nM (EC50) |
5-HT2B Receptor 431 nM (Ki) |
5-HT2C agonist-13 (compound 58) (10 pM-10 μM; 45 min) binds potently to human recombinant 5-HT2C receptors expressed in HEK293E cell membranes with a Ki of 20 nM, and shows selective binding over human 5-HT2B and 5-HT2A receptors[1].
5-HT2C agonist-13 (90 s-18 h) potently activates human recombinant 5-HT2C receptors expressed in HEK293E cells with an EC50 of 16 nM, and exhibits high functional selectivity over human 5-HT2B and 5-HT2A receptors, acting as a partial agonist at the latter two[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
5-HT2C agonist-13 (10 mg/kg; p.o.; single dose; co-administered with SB-243213) has its food intake-reducing effect in male Sprague Dawley rats fully reversed by co-administration of a selective 5-HT2C antagonist, confirming mediation via the 5-HT2C receptor[1].
5-HT2C agonist-13 (3-30 mg/kg; p.o.; daily; 4 days) reduces body weight gain in lean Sprague Dawley rats in a dose-dependent manner, with a statistically significant 6% reduction at 30 mg/kg on day 4[1].
5-HT2C agonist-13 (300 mg/kg; p.o.; single dose) does not cause gastric parietal cell necrosis or stomach lesions in mice after 24 hours[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 (male, 250 g)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Caused a 12% reduction in food pellet consumption compared to vehicle.
Caused a statistically significant 32% reduction in food pellet consumption compared to vehicle.
Caused a statistically significant 41% reduction in food pellet consumption compared to vehicle.
Left water consumption and locomotor activity within normal ranges, and no overt physical or behavioral abnormalities were observed.
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Animal Model:Sprague Dawley (male, 250 g)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose; co-administered with SB-243213
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Result:Caused a 30% reduction in food intake that was completely reversed in a dose-dependent manner by co-administration of SB-243213.
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Animal Model:Sprague Dawley (lean)[1]
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Dosage:3 mg/kg; 30 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Caused a 1.6% reduction in body weight gain compared to vehicle on day 4.
Caused a statistically significant reduction in body weight gain as early as day 2, with a 6% reduction compared to vehicle on day 4.
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Animal Model:Mice[1]
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Dosage:300 mg/kg
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Administration:p.o.; single dose
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Result:Did not cause gastric parietal cell necrosis or stomach lesions after 24 hours.
Chemical Information
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CAS No. 850033-84-0
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Molecular Weight 284.28
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Formula C14H15F3N2O
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SMILES
FC(F)(C1=C2C([C@@]3([H])N(CCNC3)C2=O)=CC(CC)=C1)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
5-HT2C agonist-13 Related Classifications
HY-182373 Related Classifications
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