Cas No.: | 821768-06-3 |
Chemical Name: | 1-Piperazinecarboxamide, 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]- |
Synonyms: | JNJ17203212;JNJ 17203212 |
SMILES: | FC(F)(F)C1=CC=CN=C1N1CCN(C(NC2C=CC(C(F)(F)F)=CN=2)=O)CC1 |
Formula: | C17H15F6N5O |
M.Wt: | 419.3243 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1. |
In 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] |