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^[1].

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 K_i 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.

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.

474.43

C₂₃H₂₁F₃N₄O₄

942614-99-5

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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 vanilloid 1 antagonist. J Pharmacol Exp Ther. 2012 Aug;342(2):520-8.  [Content Brief]

  [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.  [Content Brief]