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JTS-653

产品编号 T41091 CAS 942614-99-5

JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs.

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JTS-653, CAS 942614-99-5

规格	价格/CNY		货期	数量
25 mg	￥ 10,600		6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs.
体外活性	JTS-653 inhibits proton-induced activation of human and rat TRPV1 with IC 50 s of 0.320 and 0.347 nM, respectively[1]. JTS-653 blocks heat-induced inward currents in rat TRPV1 with an IC 50 of 1.4 nM[1]. In the competition experiments, JTS-653 displaces [ 3 H]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 IC 50 s of 0.236 and 0.247 nM, respectively[1].
体内活性	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.

分子量	474.44
分子式	C23H21F3N4O4
CAS No.	942614-99-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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. 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.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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