2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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.

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5-HT2C agonist-13

5-HT2C agonist-13 Chemical Structure

CAS No. : 850033-84-0

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5-HT2C agonist-13 Related Antibodies

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route CL Vss Tmax Cmax T1/2 AUC F
Rat[1] 4.4 mg/kg i.v. 37.4 mL/min/kg 4.8 L/kg / / / / /
Rat[1] 8.8 mg/kg p.o. / / 0.7 h 4050 nM 1.6 h 11000 nM·h 77 %
In Vivo

5-HT2C agonist-13 (compound 58) (3-30 mg/kg; p.o.; single dose) produces a dose-dependent reduction in food intake in male Sprague Dawley rats, with statistically significant 32% and 41% reductions at 10 mg/kg and 30 mg/kg, respectively[1].
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.

Animal Model: Sprague Dawley (male, 250 g)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Sprague Dawley (male, 250 g)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose; co-administered with SB-243213
Result: Caused a 30% reduction in food intake that was completely reversed in a dose-dependent manner by co-administration of SB-243213.
Animal Model: Sprague Dawley (lean)[1]
Dosage: 3 mg/kg; 30 mg/kg
Administration: p.o.; daily; 4 days
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.
Animal Model: Mice[1]
Dosage: 300 mg/kg
Administration: p.o.; single dose
Result: Did not cause gastric parietal cell necrosis or stomach lesions after 24 hours.
Molecular Weight

284.28

Formula

C14H15F3N2O
CAS No.
SMILES

FC(F)(C1=C2C([C@@]3([H])N(CCNC3)C2=O)=CC(CC)=C1)F
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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5-HT2C agonist-13 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:

5-HT2C agonist-13850033-84-05-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2C receptorobesityHEK293E cellsHEK293E cell membranesbody weight gainSB-243213Sprague Dawley rats5-HT2B receptorfood intake5-HT2A receptorInhibitorinhibitorinhibit

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