JTS-653

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JTS-653 是一种高效的选择性瞬时受体电位香草酸 1 (TRPV1) 拮抗剂。JTS-653 可减轻非甾体抗炎剂耐受产生的慢性疼痛 [1]sup>。

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.

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.. 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.Animal Model:Male Sprague-Dawley rats aged 5 to 6 weeks 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.

JTS-653 inhibits proton-induced activation of human and rat TRPV1 with IC50s of 0.320 and 0.347 nM, respectively. JTS-653 blocks heat-induced inward currents in rat TRPV1 with an IC50 of 1.4 nM. 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.JTS653 inhibits the 30 nM Capsaicin-induced activation of human and rat TRPV1 with IC50s of 0.236 and 0.247 nM, respectively.

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Others

Other Targets

TRPV1

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942614-99-5

474.43

C23H21F3N4O4

>98% (HPLC)

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(-20℃)

With Ice Pack

≥ 2 years