AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good orally bioavailable bioavailability. AM-3189 does not penetrate the rat CNS as indicated by
a rat brain to plasma ratio of 0.04 at 3 h after an orally bioavailable dose of 5 mg/kg. References:
纯度:≥98%
CAS:916219-50-6