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BCTC
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BCTC图片
CAS NO:393514-24-4
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
BCTC 是前列腺癌 (PCa) DU145 细胞中瞬时受体电位阳离子通道亚家族 M 成员 8 (TRPM8) 的强效特异性抑制剂。
Cas No.393514-24-4
别名N-(4-叔丁苯基)-4-(3-氯吡啶-2-基)哌嗪-1-甲酰胺
化学名N-(4-(tert-butyl)phenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide
Canonical SMILESClC1=CC=CN=C1N2CCN(C(NC3=CC=C(C=C3)C(C)(C)C)=O)CC2
分子式C20H25ClN4O
分子量372.89
溶解度≥ 112.6mg/mL in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.Target: TRPM8in vitro: BCTC is a potent and specific antagonist of TRPM8, exerts an anti-tumor effect on the androgen-independent PCa DU145 cells, and the mechanism of how the inhibition functions. BCTC exerts an anti-proliferative effect on DU145 cells and induces tumor suppression through G0/G1 cell cycle arrest, and inhibition of migration and invasion. BCTC demonstrates excellent anti-tumor activity in PCa DU145 cells, and therefore has the potential to become a targeted therapeutic strategy against PCa. [1]in vivo: BCTC is a potent, selective, and orally bioavailable antagonist of rat VR1. BCTC not only blocks the activation of rat VR1 by capsaicin but also by low pH at the native rat VR1 in a skin-nerve preparation. Thus, BCTC has provided us with an opportunity to test our hypothesis that the inhibition of low pH induced activation of VR1 confers in vivo efficacy in models of chronic pain. This report describes the effects of BCTC in models of inflammatory, neuropathic, and capsaicin-induced pain in the rat. The efficacy and side effect profile of BCTC in these models were compared with those of nonsteroidal anti-inflammatory drugs and antiepileptic drugs currently used for the clinical therapy of inflammatory and neuropathic pain, respectively.[2]

References:
[1]. Liu T, et al. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells. Oncol Lett. 2016 Jan;11(1):182-188.
[2]. Pomonis JD, et al. N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflamm
[3]. Valenzano KJ, et al. N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic pro