产品描述:Taranabant is a highly potent and selective
cannabinoid 1 (
CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding
Ki of 0.13 nM for the human CB1R in vitro.
IC50 & Target: IC50: 0.3 nM (hCB1R), 0.4 nM (rCB1R)
[1]
Ki: 0.13 nM (hCB1R), 0.27 nM (rCB1R)
[1] In Vitro: Taranabant (MK-0364) binds to human or rat CB1R with an IC
50 of 0.3 and 0.4 nM, respectively, corresponding to a K
i value of 0.13 and 0.27 nM, respectively. Taranabant binds to the human or rat CB2R with an IC
50 value of 290 and 470 nM, respectively, corresponding to a K
i value of 170 and 310 nM, respectively. The selectivity ratio of CB1R over CB2R is approximately 1000-fold
[1]. Taranabant (MK-0364) is a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity. IC
50s of Taranabant for CB1R and CB2R by
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