For research use only. Not for therapeutic Use.
CAY10505（Cat No.:I000834）is a highly potent and selective inhibitor of the PI3Kγ enzyme in neuronal cells, exhibiting an IC50 of 30 nM. This compound selectively targets the gamma isoform of the phosphoinositide 3-kinase (PI3Kγ) enzyme, which plays a crucial role in intracellular signaling pathways. By blocking the activity of this enzyme, CAY10505 has the potential to modulate various cellular processes and may have therapeutic applications in the treatment of neurological disorders. Its high potency and selectivity make it a promising candidate for further development.
| Catalog Number | I000834 |
| CAS Number | 1218777-13-9 |
| Synonyms | (5E)-5-[[5-(4-fluorophenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione |
| Molecular Formula | C14H8FNO3S |
| Purity | ≥95% |
| Target | Apoptosis |
| Solubility | Soluble in DMSO > 10 mM |
| Storage | Store at -20°C |
| IUPAC Name | (5E)-5-[[5-(4-fluorophenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione |
| InChI | InChI=1S/C14H8FNO3S/c15-9-3-1-8(2-4-9)11-6-5-10(19-11)7-12-13(17)16-14(18)20-12/h1-7H,(H,16,17,18)/b12-7+ |
| InChIKey | UFBTYTGRUBUUIL-KPKJPENVSA-N |
| SMILES | C1=CC(=CC=C1C2=CC=C(O2)C=C3C(=O)NC(=O)S3)F |
| Reference | 1:Can J Physiol Pharmacol. 2012 Jul;90(7):881-5. doi: 10.1139/y2012-089. Epub 2012 Jun 25. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats.Tyagi S,Sharma S,Budhiraja RD, PMID: 22731503 DOI: 10.1139/y2012-089 </br><span>Abstract:</span> This study has been designed to investigate the role of phosphatidyl-inositol 3-kinase-γ (PI3Kγ) in deoxycorticosterone acetate salt (DOCA) hypertension induced vascular endothelium dysfunction. Wistar rats were uninephrectomised and DOCA (40 mg·(kg body mass)(-1), subcutaneous injection) was administered twice weekly for 6 weeks to produce hypertension. Rats with mean arterial blood pressure ≥ 140 mm Hg (1 mm Hg = 133.322 Pa) were selected as hypertensive. Vascular endothelium dysfunction was assessed in terms of attenuation of acetylcholine-induced endothelium-dependent relaxation (isolated aortic ring preparation), decrease in serum nitrate and (or) nitrite level, as well as reduced level of glutathione and disruption of integrity of vascular endothelium (histopathology). Five weeks of DOCA administration were followed by 7 days of daily administration of PI3Kγ inhibitor (5-[[5-(4-fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione (CAY10505), 0.6 mg·kg(-1), per os (p.o.)), atorvastatin (30 mg·kg(-1), p.o.), and losartan (25 mg·kg(-1), p.o.) (positive control of hypertension), which significantly improved acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats.Therefore, it may be concluded that CAY10505, a specific inhibitor of PI3Kγ, improves hypertension-associated vascular endothelial dysfunction. Thus, inhibition of PI3Kγ might be a useful approach in the therapeutics of vascular endothelium dysfunction. |
