942614-99-5
942614-99-5 structure
- Name: Jts-653
- Chemical Name: JTS-653
- CAS Number: 942614-99-5
- Molecular Formula: C23H21F3N4O4
- Molecular Weight: 474.43
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2020-08-07 17:52:45
- Modify Date: 2024-01-23 18:18:04
-
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].
| Name | JTS-653 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Molecular Formula | C23H21F3N4O4 |
|---|---|
| Molecular Weight | 474.43 |