SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, SBFI-26 binds to the canonical ligand-binding pocket of FABP5[3],with Kjs of 0.
货号:ajcx16248
CAS:1541207-06-0
分子式:C28H22O4
分子量：422.47
溶解度:DMSO: 100 mg/mL (236.70 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, SBFI-26 binds to the canonical ligand-binding pocket of FABP5^[3],with Kjs of 0.9 μM and 0.4 μM for FABP5 and ABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects^[1,2].

The FABP inhibitor SBFI-26 does not decrease the amplitude of EPSCs and is a weak agonist of PPARα and PPARγ receptors. Confirming its selectivity for FABPs, SBFI-26failed to reduce AEA uptake in cells bearing a knockdown of FABP5, the main FABP expressed in HeLa cells. Additionally, SBFI-26 does not inhibit FAAH. Collectively, SBFI-26 is a selective FABP inhibitor^[1].

SBFI-26 produces analgesic and anti-inflammatory effects in mice, SBFI-26 (20 mg/kg) significantly reduced carrageenan-induced thermal hyperalgesia and paw edema^[1]. FABP5 was the only one dramatically upregulated along with increased protein expression in the established PH-LHD mouse model. Inhibition of FABP5 by SBFI-26 injection abrogated pulmonary artery remodelling in PH-LHD and improved cardiac function^[4].

参考文献:
[1]: Berger WT, Ralph BP, et,al. Targeting fatty acid binding protein (FABP) anandamide transporters - a novel strategy for development of anti-inflammatory and anti-nociceptive drugs. PLoS One. 2012;7(12):e50968. doi: 10.1371/journal.pone.0050968. Epub 2012 Dec 7. PMID: 23236415; PMCID: PMC3517626.
[2]: Hsu HC, Tong S, et,al. The Antinociceptive Agent SBFI-26 Binds to Anandamide Transporters FABP5 and FABP7 at Two Different Sites. Biochemistry. 2017 Jul 11;56(27):3454-3462. doi: 10.1021/acs.biochem.7b00194. Epub 2017 Jun 28. PMID: 28632393; PMCID: PMC5884075.
[3]: Hsu HC, Tong S, et,al.The Antinociceptive Agent SBFI-26 Binds to Anandamide Transporters FABP5 and FABP7 at Two Different Sites. Biochemistry. 2017 Jul 11;56(27):3454-3462. doi: 10.1021/acs.biochem.7b00194. Epub 2017 Jun 28. PMID: 28632393; PMCID: PMC5884075.
[4]: Lei Q, Yu Z, et,al. Fatty acid-binding protein 5 aggravates pulmonary artery fibrosis in pulmonary hypertension secondary to left heart disease via activating wnt/β-catenin pathway. J Adv Res. 2022 Sep;40:197-206. doi: 10.1016/j.jare.2021.11.011. Epub 2021 Nov 26. PMID: 36100327; PMCID: PMC9481948.

Protocol:

Cell experiment [1]:
Cell lines	HeLa cells
Preparation Method	Cells were transfected with the PPAR reporter system, incubated with GW7647, rosiglitazone, or SBFI-26 for 6 hrs, followed by measurement of luciferase and β-galactosidase activity using a luminometer as described.
Reaction Conditions	10uM SBFI-26 for 6 hrs
Applications	Confirming its selectivity for FABPs, SBFI-26 failed to reduce AEA uptake in cells bearing a knockdown of FABP5, the main FABP expressed in HeLa cells. Additionally, SBFI-26 does not inhibit FAAH. Collectively,SB-FI-26 is a selective FABP inhibitor.
Animal experiment [2]:
Animal models	Male C57Bl6 mice (22-30 g)
Preparation Method	SBFI-26 (20 mg/kg) was dissolved in ethanol∶emulphor∶saline (1∶1∶18), requiring sonication and gentle heating for solubilization, and administered 45 min prior to injection of carrageenan.
Dosage form	20 mg/kg SBFI-26 for 45min
Applications	SBFI-26 (20 mg/kg) significantly reduced carrageenan-induced thermal hyperalgesia and paw edema
参考文献: [1]: Berger WT, Ralph BP, et,al. Targeting fatty acid binding protein (FABP) anandamide transporters - a novel strategy for development of anti-inflammatory and anti-nociceptive drugs. PLoS One. 2012;7(12):e50968. doi: 10.1371/journal.pone.0050968. Epub 2012 Dec 7. PMID: 23236415; PMCID: PMC3517626.