Trequinsin hydrochloride |
Catalog No.GC13495 |
El clorhidrato de trequinsina (HL 725) es un inhibidor extremadamente potente de la CAMP fosfodiesterasa plaquetaria (PDE), con una IC50 de 0,25 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 78416-81-6
Sample solution is provided at 25 µL, 10mM.
Trequinsin is a phosphodiesterase (PDE) 3 inhibitor that is dependent on cyclic AMP (cAMP), with IC50 values of 0.04 and 0.03 nM for PDE3A and PDE3B, respectively, in T84 human colonic adenocarcinoma cell lysates.[1] In cultured primary rat juxtaglomerular cells, trequinsin stimulates cAMP accumulation when used at a concentration of 10 µM and increases cell membrane capacitance in a patch clamp assay.[2] Trequinsin also competitively inhibits the multidrug resistant protein 5-mediated export of cGMP from Chinese hamster lung fibroblasts with a Ki value of 240 nM.[3] In vivo, trequinsin reduces collagen-induced platelet aggregation in rabbits when administered intravenously at a rate of 3 µg/kg per minute, as well as the collagen-induced decrease in mean arterial blood pressure when administered alone or in combination with prostacyclin.[4]
Reference:
[1]. Liu, S., Veilleux, A., Zhang, L., et al. Dynamic activation of cystic fibrosis transmembrane conductance regulator by type 3 and type 4D phosphodiesterase inhibitors. J. Pharmacol. Exp. Ther. 314(2), 846-854 (2005).
[2]. Friis, U.G., Jensen, B.L., Sethi, S., et al. Control of renin secretion from rat juxtaglomerular cells by cAMP-specific phosphodiesterases. Circ. Res. 90(9), 996-1003 (2002).
[3]. Jedlitschky, G., Burchell, B., and Keppler, D. The multidrug resistance protein 5 functions as an ATP-dependent export pump for cyclic nucleotides. J. Biol. Chem. 275(39), 30069-30074 (2000).
[4]. Darius, H., Lefer, A.M., Leprán, I., et al. In vivo interaction of prostacyclin with an inhibitor of cyclic nucleotide phosphodiesterase, HL 725. Br. J. Pharmacol. 84(3), 735-741 (1985).
Average Rating: 5
(Based on Reviews and 11 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *