货号 | 3361/50 |
别名 | 4-[3-(Trifluoromethyl)-2-pyridinyl] |
供应商 | Tocris |
生物活性 | Reversible, competitive and potent TRPV1 antagonist (pKi values are 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively). Inhibits capsaicin- and H+-induced channel activation (pIC50 values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 419.32 |
分子式 | C17H15F6N5O |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
CAS号 | 821768-06-3 |
参考文献 | Bhattacharyaet al (2007) Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J.Pharmacol.Exp.Ther. 323 665. PMID: 17690251. Ghilardiet al (2005) Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J.Neurosci. 25 3126. PMID: 15788769. Swansonet al (2005) Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J.Med.Chem. 48 1857. PMID: 15771431. |