AF38469

AF38469 is a novel, selective, orally bioavailable Sortilin inhibitor with an IC50 value of 330 nM.

Signaling Pathways >> Others >> Others

Research Areas >> Others

IC50:330 nM (Sortilin)[1]

AF38469 showed no inhibition or stimulation of >50% at 10 μM 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].

[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.

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