| Identification | Back Directory | [Name]
CAY10505 | [CAS]
1218777-13-9 | [Synonyms]
CAY10505
CAY10505, >=98%
CAY10505 USP/EP/BP
(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
(5E)-5-[[5-(4-Fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 5-[[5-(4-fluorophenyl)-2-furanyl]methylene]-, (5E)-
CAY10505 ( 5E)-5-[[5-(4-Fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione | [Molecular Formula]
C14H8FNO3S | [MDL Number]
MFCD00640727 | [MOL File]
1218777-13-9.mol | [Molecular Weight]
289.28 |
| Chemical Properties | Back Directory | [density ]
1.466 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥14.45 mg/mL in DMSO | [form ]
solid | [pka]
7.21±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
CAY10505 is a phosphoinositide 3-kinase gamma (PI3Kγ) specific inhibitor and improves hypertension-associated vascular endothelial dysfunction. | [Biological Activity]
cay10505 is a potent and selective pi3kγ inhibitor (ic50= 30 nm)pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in neurons treated with 3.5 μm ba, 200 nm cay10505 partially reduced the baicalein-induced akt phosphorylation. [1]in hypertensive rats, cay10505 at 0.6 mg.kg-1 p.o. exhibited the following effects 1) effectively reduced mabp; 2) significantly ameliorated vascular endothelium dysfunction in hypertensive rats in combination of doca; 3) prominently increased serum nitrite and/or nitrate concentrations.4) prevented hypertension-induced attenuation of ach-induced endothelium-dependent relaxation.[2] | [in vivo]
Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation[3]. | [IC 50]
PI3Kγ: 30 nM (IC50, Neurons) | [References]
[1] tyagi s, sharma s, budhiraja rd. effect of phosphatidylinositol 3-kinase-γ inhibitor cay10505 in hypertension, and its associated vascular endothelium dysfunction in rats. can j physiol pharmacol. 2012 jul;90(7):881-5.
[2] sun yy, lin sh, lin hc et al. cell type-specific dependency on the pi3k/akt signaling pathway for the endogenous epo and vegf induction by baicalein in neurons versus astrocytes. plos one. 2013 jul 19;8(7):e69019. |
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