1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. JTS-653

JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.

For research use only. We do not sell to patients.

JTS-653 Chemical Structure

JTS-653 Chemical Structure

CAS No. : 942614-99-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents[1].

IC50 & Target[1]

TRPV1

 

In Vitro

JTS-653 inhibits proton-induced activation of human and rat TRPV1 with IC50s of 0.320 and 0.347 nM, respectively[1]. JTS-653 blocks heat-induced inward currents in rat TRPV1 with an IC50 of 1.4 nM[1].
In the competition experiments, JTS-653 displaces [3H]RTX binding to human and rat TRPV1 in a concentration-related manner with Ki values of 11.44 and 4.40 nM, respectively[1].
JTS653 inhibits the 30 nM Capsaicin-induced activation of human and rat TRPV1 with IC50s of 0.236 and 0.247 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JTS-653 significantly prevents Capsaicin-induced mechanical hyperalgesia at 1 mg/kg p.o. and attenuates Carrageenan-induced mechanical hyperalgesia at 0.3 mg/kg p.o. JTS-653 significantly attenuates Carrageenan-induced thermal hyperalgesia at 0.1 mg/kg p.o. and fully reverses at 0.3 mg/kg p.o. without affecting the volume of the Carrageenan-treated paw. JTS-653 shows a transient increase of body temperature at 0.3 mg/kg p.o.[1].
JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents in rats and mice including post-herpetic pain. JTS-653 (0.3, 1, 3 mg/kg) shows its effect in a dose-related manner, with statistical significance at 0.3 mg/kg or above[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats aged 5 to 6 weeks[2]
Dosage: 0.3, 1, 3 mg/kg
Administration: 0.5 h, 2 h, 8 h, 25 h
Result: Partially attenuated mechanical hyperalgesia in the L5 spinal nerve ligation model in rats at 0.3 mg/kg.
Increased the paw withdrawal threshold (PWT) of the ipsilateral paw at 0.5, 2, and 8 h after the administration and its effect disappeared by 25 h after administration.
Showed its maximum effect with 1 mg/kg at 2 h after administration.
Molecular Weight

474.43

Formula

C23H21F3N4O4

CAS No.
SMILES

OC[C@@H]1N(C(N=C2)=CC=C2C)C3=CC=CC(C(NC(C=C4)=CN=C4OCC(F)(F)F)=O)=C3OC1

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.
  • 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JTS-653
Cat. No.:
HY-19589
Quantity:
MCE Japan Authorized Agent: