- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: SP-13786
- Price:
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Huang
- DC Chemicals Limited
- China
- Product Name: UAMC-1110
- Price: $850.0/100mg $1350.0/250mg $2700.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
1448440-52-5
1448440-52-5 structure
- Name: SP-13786
- Chemical Name: SP-13786
- CAS Number: 1448440-52-5
- Molecular Formula: C17H14F2N4O2
- Molecular Weight: 344.315
- Catalog: Research Areas Cancer
- Create Date: 2018-04-14 05:05:49
- Modify Date: 2024-01-10 08:10:33
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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.
| Name | SP-13786 |
|---|---|
| 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 |
| 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 |
| 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℃ |