170686-10-9Relevant articles and documents
BMS-196085: A potent and selective full agonist of the human β3 adrenergic receptor
Gavai,Sher,Mikkilineni,Poss,McCann,Girotra,Fisher,Wu,Bednarz,Mathur,Wang,Sun,Slusarchyk,Skwish,Allen,Hillyer,Frohlich,Abboa-Offei,Cap,Waldron,George,Tesfamariam,Harper,Ciosek Jr.,Young,Dickinson,Seymour,Arbeeny,Washburn
, p. 3041 - 3044 (2007/10/03)
A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human β3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent β3 full agonist (Ki=21 nM, 95% activation) with partial agonist (45%) activity at the β1 receptor. Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation.