CB1-IN-1 Inhibitor

CB1-IN-1 is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3nM and 21nM,respectively.

1. Chang C P, Wu C H, Song J S, et al. Discovery of 1- (2,4-dichlorophenyl)-N- (piperidin-1-yl)-4- ((pyrrolidine-1-sulfonamido)methyl)-5- (5- ((4- (trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice.[J]. Journal of Medicinal Chemistry, 2013, 56 (24):9920.
2. Chang C P, Huang H L, Huang J K, et al. Fluorine-18 Isotope Labeling for Positron Emission Tomography Imaging. Direct Evidence for DBPR211 as a Peripherally Restricted CB1 Inverse Agonist[J]. Bioorganic & Medicinal Chemistry, 2018.

Small volumes of CB1-IN-1, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5752260 is an inhibitor targeting CB1-IN-1.