A nucleotide and dual P2Y2 and P2Y4 receptor agonist
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Uridine 5'-triphosphate (UTP) is a nucleotide and dual agonist of purinergic P2Y2 and P2Y4 receptors (EC50s = 55 and 80 nM, respectively, for stimulation of phospholipase C in 1321N1 cells expressing human receptors).1,2 It is selective for P2Y2 and P2Y4 receptors over P2Y6 receptors (EC50 = >10,000 nM).2 UTP stimulates proliferation of PANC-1 cells (EC50 = 13.1 μM), an effect that can be prevented by siRNA against the P2Y2 receptor.1 It induces vasoconstriction in perfused isolated canine epicardial coronary artery in a concentration-dependent manner.3 UTP is formed from uridine monophosphate (UMP) by two sequential phosphorylations and can be converted to cytidine 5'-triphosphate .4 It also reacts with glucose-1-phosphate to form UDP-glucose , a precursor in the biosynthesis of glycogen.5
1.Choi, J.H., Ji, Y.G., and Lee, D.H.Uridine triphosphate increases proliferation of human cancerous pancreatic duct epithelial cells by activating P2Y2 receptorPancreas42(4)680-686(2013) 2.Maruoka, H., Jayasekara, M.P.S., Barrett, M.O., et al.Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y4 receptorJ. Med. Chem.54(12)4018-4033(2011) 3.Matsumoto, T., Nakane, T., and Chiba, S.UTP induces vascular responses in the isolated and perfused canine epicardial coronary artery via UTP-preferring P2Y receptorsBr. J. Pharmacol.122(8)1625-1632(1997) 4.Berg, J.M., Tymoczko, J.L., and Stryer, L.In de novo synthesis, the pyrimidine ring is assembled from bicarbonate, aspartate, and glutamineBiochemistry(2002) 5.Berg, J.M., Tymoczko, J.L., and Stryer, L.Glycogen is synthesized and degraded by different pathwaysBiochemistry(2002)
3'-Azido-3'-deoxythymidine β-D-glucuronide (sodium salt)
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