5-HT2C-agonist-14
5-HT2C-agonist-14 is a 5-HT2C receptor agonist with an EC50 of 2.9 μM against human receptors. It also acts as a voltage-gated sodium channel inhibitor with blood-brain barrier permeable. 5-HT2C-agonist-14 elevates seizure threshold, suppresses seizure progression and alleviates pain-related behaviors. It can be used in the research of epilepsy and pain-related diseases.
For research use only. We do not sell to patients.
- CAS No.: 3091546-67-4
- Formula: C17H22F3N3O4
- Molecular Weight:389.37
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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
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Biological Activity
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Human 5-HT2C Receptor 2.9 μM (EC50) |
5-HT2C-agonist-14 ((R)-46) (0.1-100 μM; 72 h) exhibits low in vitro hepatotoxicity in HepG2 cells, and only significantly reduces cell viability after treatment at 100 μM for 72 h[1].
5-HT2C-agonist-14 (10 μM) binds tightly to site 2 of voltage-gated sodium channels in rat cerebral cortex cell membranes, and inhibits 73.6% of control-specific binding[1].
5-HT2C-agonist-14 (10 μM) acts as a potent agonist for the human 5-HT2C receptor in recombinant HEK-293 cells, with an EC50 of 2.9 μM and an agonist response rate of 77.6% at 10 μM[1].
5-HT2C-agonist-14 (250 μM) preferentially inhibits voltage-gated sodium channels in fast-inactivation and slow-inactivation states in N1E-115 neuroblastoma cells, with a stronger inhibitory effect on slow-inactivation channels[1].
5-HT2C-agonist-14 exhibits excellent passive membrane permeability in the PAMPA assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:0.1, 1, 10, 25, 50, 100 μM
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Incubation Time:72 h
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Result:Did not significantly reduce cell viability at concentrations from 0.1 μM to 50 μM.
Caused a statistically significant reduction in cell viability at 100 μM.
| Species | Dose | Route | Tmax (Brain) | Cmax (Brain) | T1/2 (Brain) | AUC0-∞ (Brain) |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.v. | 5 min | 6716.67 ng/g | 26.41 min | 169977.7 min·ng/mL |
| Mice[1] | 25 mg/kg | p.o. | 5 min | 5625.83 ng/g | 93.31 min | 353003.8 min·ng/mL |
| Mice[1] | 25 mg/kg | i.p. | 5 min | 17441.67 ng/g | 75.02 min | 546628.0 min·ng/mL |
| Mice[1] | 50 mg/kg | i.p. | 5 min | 33433.33 ng/g | 55.86 min | 1823614.1 min·ng/mL |
Chemical Information
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CAS No. 3091546-67-4
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Molecular Weight 389.37
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Formula C17H22F3N3O4
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SMILES
FC(F)(F)OC1=CC=CC(N2CCN(CC2)C([C@@H](COC)NC(C)=O)=O)=C1
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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-14 Related Classifications
HY-183652 Related Classifications
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