SP-13786 |
Catalog No.GC19425
One-Click Copy Product Info
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SP-13786 is a potent and highly selective inhibitor of fibroblast activation protein (FAP) and prolyl oligopeptidase (PREP) (FAP: IC50 = 3.2nM; PREP: IC50 = 1.8μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448440-52-5
Sample solution is provided at 25 µL, 10mM.
SP-13786 is a potent and highly selective inhibitor of fibroblast activation protein (FAP) and prolyl oligopeptidase (PREP) (FAP: IC50 = 3.2nM; PREP: IC50 = 1.8μM) [1]. SP-13786 inhibits FAP's serine protease activity by binding to its catalytic site, thereby inhibiting FAP's function in tumor stroma or fibrotic tissue [2]. SP-13786 is used to study the role of FAP in tumors, fibrosis, and other pathological processes [3-4].
In MGC803 cells, Co-incubation with SP-13786 (10μM; 24h) significantly reduced the antitumor activity of cresyl violet (CV)-FAP [5]. In U87MG-Fluc cells, SP-13786 (50μM, 100μM; 30min) reduces intracellular FAP levels [6].
In BALB/c mice, SP-13786 (10mg/kg; iv; signle injection) targets and inhibits FAPα activity [7]. In myocardial infarction (MI) mouse model, SP-13786 (0.5mg/kg; ip; 7d) inhibits FAP and significantly improves cardiac function and promotes angiogenesis after MI [8].
References:
[1]. Jansen K, Heirbaut L, Verkerk R, et al. Extended structure–activity relationship and pharmacokinetic investigation of (4-quinolinoyl) glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP)[J]. Journal of medicinal chemistry, 2014, 57(7): 3053-3074.
[2]. Kiani M, Jokar S, Hassanzadeh L, et al. Recent clinical implications of FAPI: imaging and therapy[J]. Clinical nuclear medicine, 2022: 10.1097.
[3]. Butuzova D A, Kulebyakina M A, Basalova N A, et al. Fibroblast Activation Protein Alpha (FAPα) as a Promising Target in the Diagnostics and Treatment of Cancer and Fibrotic Diseases: Recent Approaches to Imaging and Assessment of Functional Activity[J]. Biochemistry (Moscow), 2025, 90(Suppl 1): S135-S145.
[4]. Zhou Y, Yin K, Dong H, et al. Long-lasting bioluminescence imaging of the fibroblast activation protein by an amphiphilic block copolymer-based probe[J]. Analytical Chemistry, 2021, 93(8): 3726-3732.
[5]. Liu S Y, Wang H, Nie G. Ultrasensitive fibroblast activation protein-α-activated fluorogenic probe enables selective imaging and killing of melanoma in vivo[J]. ACS sensors, 2022, 7(7): 1837-1846.
[6]. Lin Y, Ma Z, Li Z, et al. Bioluminescent probe for monitoring endogenous fibroblast activation protein-alpha[J]. Analytical Chemistry, 2019, 91(23): 14873-14878.
[7]. Fu A, Wang H, Huo T, et al. A novel chemiluminescence probe for sensitive detection of fibroblast activation protein-alpha in vitro and in living systems[J]. Analytical Chemistry, 2021, 93(16): 6501-6507.
[8]. Sun Y, Ma M, Cao D, et al. Inhibition of fap promotes cardiac repair by stabilizing BNP[J]. Circulation research, 2023, 132(5): 586-600.
| Cell experiment [1]: | |
Cell lines | MGC803 cells |
Preparation Method | For cell cytotoxicity assay, cells were previously seeded on 96-well plates at a density of 1 × 104 per well in 200μL of culture medium; after 16h, the culture medium was removed, and fresh serum-free culture medium containing different dosages of cresyl violet (CV)-FAP, cresyl violet, or SP-13786 together with CV-FAP was added. After incubation for 24h, 20μL of cell counting kit-8 (CCK-8) was added to each well and incubated at 37℃ for 2h; the absorbance intensity at 450nm was recorded using a multifunctional microplate reader. |
Reaction Conditions | 10μM; 24h |
Applications | Co-incubation with SP-13786 significantly reduced the antitumor activity of CV-FAP. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | BALB/c mice were divided into two groups randomly and anesthetized with 3% isoflurane in 97% oxygen gas. To estimate the distribution and clearance of probe CFCL and the inhibition effect of SP-13786 on FAPα in the whole animal level, the mice were treated with probe CFCL intravenously (200μM, 100μL) with or without the pretreating of SP-13786 in saline (10mg/kg, i.v.). The images of each mouse were recorded with 1min exposure time. |
Dosage form | 10mg/kg; iv; signle injection |
Applications | SP-13786 targets and inhibits FAPα activity. |
References: | |
| Cas No. | 1448440-52-5 | SDF | |
| 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 | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9043 mL | 14.5214 mL | 29.0428 mL |
| 5 mM | 580.9 μL | 2.9043 mL | 5.8086 mL |
| 10 mM | 290.4 μL | 1.4521 mL | 2.9043 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)