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

JTS-653 

Cat. No.: HY-19589
Handling Instructions

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

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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].

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].

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.

942614-99-5

SMILES

OC[[email protected]@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.

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Keywords:

JTS-653JTS653JTS 653TRP ChannelTransient receptor potential channelstransientreceptorpotentialvanilloidTRPV1non-steroidalanti-inflammatoryNSAIDchronicpainInhibitorinhibitorinhibit

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JTS-653
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HY-19589
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