AF38469 is a selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.
in vivo
AF38469 (1 mg/kg; i.v.) has a low volume of distribution (blood volume of 0.7 L/kg) and low clearance (4.8 L/h/kg), and a half-life (t1/2) of 1.2 h in rat[1].
References
[1] Schroder TJ, et al. The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorg Med Chem Lett. 2014 Jan 1;24(1):177-80. DOI:10.1016/j.bmcl.2013.11.046
