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SP-13786 Catalog No.GC19425

FAP-IN-1 is fibroblast activation protein (FAP) inhibitor

Size Price Stock Qty
10mM*1mL in DMSO
$127.00
In stock
2mg
$67.00
In stock
5mg
$121.00
In stock
10mg
$187.00
In stock
25mg
$388.00
In stock
50mg
$656.00
In stock
100mg
$1,071.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Animal experiment:

Rats: The PK parameters are determined for inhibitors 4, 5, 60 (SP-13786), and 61 in rats. Six male rats are treated for each inhibitor tested, three of which received the compound via a single intravenous (iv) administration at 5 mg/kg. The other three animals are dosed per os (po) at 20 mg/kg. Blood samples are collected at 0.083, 0.25, 0.5, 1, 2, 4, 6, and 24 h after administration. Inhibitor concentrations are determined using UPLC−MS/MS, and pharmacokinetic parameters are calculated using standard algorithms[1].

References:

[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.

Chemical Properties

Cas No. 1448440-52-5 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES O=C(C1=CC=NC2=CC=CC=C12)NCC(N3[C@H](C#N)CC(F)(F)C3)=O
Formula C17H14F2N4O2 M.Wt 344.32
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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.