2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. 5-HT Receptor Sodium Channel
  4. 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.

5-HT2C-agonist-14

5-HT2C-agonist-14 Chemical Structure

CAS No. : 3091546-67-4

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

5-HT2C-agonist-14 Related Antibodies

Top Publications Citing Use of Products

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

View All Sodium Channel Isoform Specific Products:

View All Isoforms
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

Human 5-HT2C Receptor

2.9 μM (EC50)

In Vitro

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.

5-HT2C-agonist-14 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2
Concentration: 0.1, 1, 10, 25, 50, 100 μM
Incubation Time: 72 h
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.
Parmacokinetics
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
Molecular Weight

389.37

Formula

C17H22F3N3O4
CAS No.
SMILES

FC(F)(F)OC1=CC=CC(N2CCN(CC2)C([C@@H](COC)NC(C)=O)=O)=C1
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

5-HT2C-agonist-14 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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-143091546-67-45-HT ReceptorSodium ChannelSerotonin Receptor5-hydroxytryptamine ReceptorNa channelsNa+ channelsdiabetic neuropathy5-HT2C receptorHepG2 cellsvoltage-gated sodium channelSH-SY5Y cellsepilepsypain-related disordersHEK-293 cellsblood-brain barrierchemotherapy-induced peripheral neuropathyInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
5-HT2C-agonist-14
Cat. No.:
HY-183652
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.