| Bioactivity | SP-13786 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. | ||||||||||||
| Target | IC50: 3.2 nM (FAP), 1.8 μM (PREP) | ||||||||||||
| Invitro | SP-13786 is also found to have better FAP/PREP selectivity and a very proficient ligand efficiency of 0.34. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SP-13786 相关抗体: | ||||||||||||
| In Vivo | SP-13786 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 SP-13786 demonstrates high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
| CAS | 1448440-52-5 | ||||||||||||
| Formula | C17H14F2N4O2 | ||||||||||||
| Molar Mass | 344.32 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
SP-13786
CAS: 1448440-52-5 F: C17H14F2N4O2 W: 344.32
SP-13786 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM; also
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