2017年12月3日星期日

SP-13786|cas 1448440-52-5

SP-13786|cas 1448440-52-5

DC Chemicals, Website: www.dcchemicals.com

Product Name: SP-13786|Cas Number: 1448440-52-5| Catalog Number: DC10416|Other Nmaes: SP13786; SP 13786

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].

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