product name CAY10505
Description: CAY10505, the dehydroxyl form of AS-252424, is a PI3Kγ inhibitor with IC50 of 33 nM. CAY10505 is a phosphatidylinositol 3-kinase-γ inhibitor , was found to significantly improve acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. CAY10505 , may improve hypertension-associated vascular endothelial dysfunction. Inhibition of PI3Kγ might be a useful approach in the therapeutics of vascular endothelium dysfunction.
References: Can J Physiol Pharmacol. 2012 Jul;90(7):881-5.
289.28
Formula
C14H8FNO3S
CAS No.
1218777-13-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 58 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Chemical Name
(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
other peoduct :
| In Vitro | Kinase Assay:
Cell Assay: In neurons treated with 3.5 μM BA, 200 nM CAY10505 partially reduced the baicalein-induced Akt phosphorylation. |
|---|---|
| In Vivo | 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. |
| Animal model | |
| Formulation & Dosage | |
| References | [1] Can J Physiol Pharmacol. 2012 Jul;90(7):881-5; [2] PLoS One. 2013 Jul 19;8(7):e69019. |
