| Bioactivity | 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]. |
| Invitro | 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: |
| Name | JTS-653 |
| CAS | 942614-99-5 |
| Formula | C23H21F3N4O4 |
| Molar Mass | 474.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yoshihiro Kitagawa, et al. Pharmacological characterization of (3S)-3-(hydroxymethyl)-4-(5-methylpyridin-2-yl)-N-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-3,4-dihydro-2H-benzo[b][1,4]oxazine-8-carboxamide (JTS-653), a novel transient receptor potential vani [2]. Yoshihiro Kitagawa, et al. Orally administered selective TRPV1 antagonist, JTS-653, attenuates chronic pain refractory to non-steroidal anti-inflammatory drugs in rats and mice including post-herpetic pain. J Pharmacol Sci. 2013;122(2):128-37. |
JTS-653
CAS: 942614-99-5 F: C23H21F3N4O4 W: 474.43
JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in viv
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