JNJ 17203212 是一种选择性、有效和竞争性的 TRPV1 拮抗剂。
| Cas No. | 821768-06-3 |
| 别名 | 4-(3-(三氟甲基)吡啶-2-基)-N-(5-三氟甲基)吡啶-2-基)哌嗪-1-甲酰胺 |
| 化学名 | 4-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-carboxamide |
| Canonical SMILES | FC(F)(C1=CC=CN=C1N2CCN(C(NC3=NC=C(C(F)(F)F)C=C3)=O)CC2)F |
| 分子式 | C17H15F6N5O |
| 分子量 | 419.32 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.IC50 value: 65 nM (human TRPV1), 102 nM (rat TRPV1)Target: TRPVin vivo: JNJ-17203212 reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. Throughout this study, colonic sensitivity was assessed via quantification of VMR to CRD in rats following a single, oral administration of JNJ-17203212 (3, 10 or 30 mg/kg) or vehicle. [1] Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents core hypothermia evoked by sc capsaicin. Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents capsaicin-evoked hypothermia in a dose-response manner. [2] References:
[1]. Wiskur BJ, et al. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats. Methods Find Exp Clin Pharmacol. 2010 Oct;32(8):557-64.
[2]. Swanson DM, et al. 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. 2005 Mar 24;48(6):185 |
