| 货号 | 17555-5mg |
| 描述 | Cholecystokinin (CCK) is a peptide hormone that, through specific receptors, induces pancreatic growth and enzyme secretion, smooth muscle contraction in the gall bladder and stomach, and modulates feeding and behavior.1,2,3 Lorglumide is a nonpeptidic antagonist of the CCK A receptor (CCK1; IC50 = 50 nM) that is 60-fold less effective at the CCK B receptor (CCK2; IC50 = 3 µM).4 It blocks CCK-mediated gut muscle contraction, pancreatic growth, and pancreatic secretion.5,6,7 Lorglumide is commonly used to study the roles of CCK1 in tissues and in animals.8,9 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sabbatini, M.E.,Chen, X.,Ernst, S.A., et al. Rap1 activation plays a regulatory role in pancreatic amylase secretion. The Journal of Biological Chemisty (2008). 2.Murphy, K.G., and Bloom, S.R. Gut hormones in the control of appetite. Experimental Physiology 89(5), 507-516 (2004). 3.Wynne, K.,Stanley, S., and Bloom, S. The gut and regulation of body weight. Journal of Clinical Endocrinology and Metabolism 89(6), 2576-2582 (2004). 4.Makovec, F.,Peris, W.,Revel, L., et al. Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives. Journal of Medicinal Chemistry 35(1), 28-38 (1992). 5.Barthó, L.,Holzer, P.,Lembeck, F., et al. Evaluation of a new and potent cholecystokinin antagonist on motor responses of the guinea-pig intestine. Br.J.Pharmac. 90, 753-761 (1987). 6.Niederau, C.,Liddle, R.A.,Williams, J.A., et al. Pancreatic growth: Interaction of exogenous cholecystokinin, a protease inhibitor, and a cholecystokinin receptor antagonist in mice. Gut 28, 63-69 (1987). 7.Scarpignato, C.,Varga, G.,Dobronyi, I., et al. Effect of a new potent CCK antagonist, lorglumide, on caerulein- and bombesin-induced pancreatic secretion and growth in the rat. British Journal of Pharmacology 96, 661-669 (1989). 8.Gamble, J.,Kenny, S., and Dockray, G.J. Plasminogen activator inhibitor (PAI)-1 suppresses inhibition of gastric emptying by cholecystokinin (CCK) in mice. Regulatory Peptides 185, 9-13 (2013). 9.Lo, C.C.,Davidson, W.S.,Hibbard, S.K., et al. Intraperitoneal CCK and fourth-intraventricular Apo AIV require both peripheral and NTS CCK1R to reduce food intake in male rats. Endocrinology 155(5), 1700-1707 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 481.4 |
| 分子式 | C22H31Cl2N2O4 • Na |
| CAS号 | 1021868-76-7 |
| 稳定性 | ≥ 2 years |
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