FAP-IN-1 is?fibroblast activation protein (FAP) inhibitor?
CAS：1448440-52-5
分子式：C17H14F2N4O2
分子量：344.32
纯度：98%
存储：Store at -20°C

Background:

FAP-IN-1 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM; also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM.

FAP-IN-1 is also found to have better FAP/PREP selectivity and a very proficient ligand efficiency of 0.34.

FAP-IN-1 is the most extensive and prolonged inhibitior of FAP in the PK studies. No tight binding behavior is observed, and the inhibitor proves to bind reversibly to FAP. Pharmacokinetic evaluation in mice of FAP-IN-1 demonstrates high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo[1].

[1]. Jansen K, et al. Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). J Med Chem. 2014 Apr 10;57(7):3053-74.