Biological Activity |
AF38469 is a novel, selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM. IC50 & Target: IC50:330 nM (Sortilin)[1] In Vitro: AF38469 showed no inhibition or stimulation of >50% at 10 uM in a standard selectivity panel of ca. 70 targets run at CEREP. Importantly AF38469 showed no activity against the NTR1 receptor. In addition AF38469 showed no activity against a selected panel of targets known to bind acidic molecules (d-Opioid, GPR40, PPARd, EP1, Angiotensin AT1, Endothelin ETA & B, MMP-12). AF38469 will serve as an important tool to further delineate the biology of Sortilin, and to facilitate evaluation of the therapeutic potential of this protein[1]. |