Molecular structure of FABP4 Inhibitor, CAS Number: 300657-03-8
FABP4 Inhibitor (CAS 300657-03-8)
See product citations (2)
Alternate Names:
2-((2′-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)-[1,1′-biphenyl]-3-yl)oxy)acetic acid
Application:
FABP4 Inhibitor is a potent and selective inhibitor of adipocyte Fatty-Acid-Binding Protein
CAS Number:
300657-03-8
Purity:
97%
Molecular Weight:
474.56
Molecular Formula:
C31H26N2O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
FABP4 Inhibitor is a cell-permeable biphenylazolo-oxyacetate that acts as a potent and selective inhibitor of A-FABP (adipocyte Fatty-Acid-Binding Protein) by targeting its fatty acid-binding pocket (Ki = < 2 nM in a competitive binding assay using 1,8-ANS), while exhibiting much lower affinity for muscle and epidermal FABP′s (Ki = 250 nM and 350 nM, respectively). FABP4 Inhibitor (A-FABP Inhibitor) may act to effectively block foam cell transformation and the cellular expression of inflammatory mediators in aP2-positive, but not aP2-negative, THP-1 macrophage in vitro, as well as improve the glucose metabolism and insulin sensitivity. It effectively binds to the fatty acid-binding pocket of FABP4 with a Ki value of less than 2 nM.
FABP4 Inhibitor (CAS 300657-03-8) References
- Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). | Sulsky, R., et al. 2007. Bioorg Med Chem Lett. 17: 3511-5. PMID: 17502136
- Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2. | Furuhashi, M., et al. 2007. Nature. 447: 959-65. PMID: 17554340
- FABP4 attenuates PPARγ and adipogenesis and is inversely correlated with PPARγ in adipose tissues. | Garin-Shkolnik, T., et al. 2014. Diabetes. 63: 900-11. PMID: 24319114
- Pimozide, a novel fatty acid binding protein 4 inhibitor, promotes adipogenesis of 3T3-L1 cells by activating PPARγ. | Wang, Y., et al. 2015. ACS Chem Neurosci. 6: 211-8. PMID: 25437245
- FABP4 inhibition suppresses PPARγ activity and VLDL-induced foam cell formation in IL-4-polarized human macrophages. | Boss, M., et al. 2015. Atherosclerosis. 240: 424-30. PMID: 25897794
- Fatty Acid-Binding Protein 4 mediates apoptosis via endoplasmic reticulum stress in mesangial cells of diabetic nephropathy. | Yao, F., et al. 2015. Mol Cell Endocrinol. 411: 232-42. PMID: 25958041
- Adipokine FABP4 integrates energy stores and counterregulatory metabolic responses. | Prentice, KJ., et al. 2019. J Lipid Res. 60: 734-740. PMID: 30705117
- FABP4 contributes to renal interstitial fibrosis via mediating inflammation and lipid metabolism. | Qiao, Y., et al. 2019. Cell Death Dis. 10: 382. PMID: 31097687
- Adipocyte-Induced FABP4 Expression in Ovarian Cancer Cells Promotes Metastasis and Mediates Carboplatin Resistance. | Mukherjee, A., et al. 2020. Cancer Res. 80: 1748-1761. PMID: 32054768
- FABP4 deactivates NF-κB-IL1α pathway by ubiquitinating ATPB in tumor-associated macrophages and promotes neuroblastoma progression. | Miao, L., et al. 2021. Clin Transl Med. 11: e395. PMID: 33931964
- Tumor resistance to ferroptosis driven by Stearoyl-CoA Desaturase-1 (SCD1) in cancer cells and Fatty Acid Biding Protein-4 (FABP4) in tumor microenvironment promote tumor recurrence. | Luis, G., et al. 2021. Redox Biol. 43: 102006. PMID: 34030117
- FABP4 activates the JAK2/STAT2 pathway via Rap1a in the homocysteine-induced macrophage inflammatory response in ApoE-/- mice atherosclerosis. | Xu, L., et al. 2022. Lab Invest. 102: 25-37. PMID: 34725437
- Targeted Inhibition of LPL/FABP4/CPT1 fatty acid metabolic axis can effectively prevent the progression of nonalcoholic steatohepatitis to liver cancer. | Yang, H., et al. 2021. Int J Biol Sci. 17: 4207-4222. PMID: 34803493
- A hormone complex of FABP4 and nucleoside kinases regulates islet function. | Prentice, KJ., et al. 2021. Nature. 600: 720-726. PMID: 34880500
- FABP4 secreted by M1-polarized macrophages promotes synovitis and angiogenesis to exacerbate rheumatoid arthritis. | Guo, D., et al. 2022. Bone Res. 10: 45. PMID: 35729106
Inhibitor of:
A-FABP, ACSL, ACSL4, AP2, CYP26B1, FABP12, FADS2, L-FABP, LOC645485, and MDGI.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
FABP4 Inhibitor, 5 mg | sc-202606 | 5 mg | $208.00 |