SP-13786

Modify Date: 2024-01-10 08:10:33

SP-13786 Structure
SP-13786 structure
 Common Name SP-13786
CAS Number 1448440-52-5 Molecular Weight 344.315
Density 1.4±0.1 g/cm3 Boiling Point 676.4±55.0 °C at 760 mmHg
Molecular Formula C17H14F2N4O2 Melting Point N/A
MSDS N/A Flash Point 362.9±31.5 °C

 Use of 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.

 Names

Name SP-13786
Synonym More Synonyms

 SP-13786 Biological Activity

Description 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.
Related Catalog
Target

IC50: 3.2 nM (FAP), 1.8 μM (PREP)[1]

In Vitro FAP-IN-1 is also found to have better FAP/PREP selectivity and a very proficient ligand efficiency of 0.34.
In Vivo 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].
Animal Admin Rats: The PK parameters are determined for inhibitors 4, 5, 60 (FAP-IN-1), 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 & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 676.4±55.0 °C at 760 mmHg
Molecular Formula C17H14F2N4O2
Molecular Weight 344.315
Flash Point 362.9±31.5 °C
Exact Mass 344.108490
LogP 0.22
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.621
Storage condition 2-8℃

 Synonyms

4-Quinolinecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-
N-{2-[(2S)-2-Cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl}-4-quinolinecarboxamide
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Chemsrc provides SP-13786(CAS#:1448440-52-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of SP-13786 are included as well.>> amp version: SP-13786

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