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Lorglumide(sodium salt)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Lorglumide(sodium salt)图片
CAS NO:1021868-76-7
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Lorglumide (sodium salt) (CR-1409 sodium salt) 是一种有效的胆囊收缩素 (CCK) 受体拮抗剂。
Cas No.1021868-76-7
别名CR-1409 sodium salt
化学名4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxo-pentanoic acid, monosodium salt
Canonical SMILESClC1=C(Cl)C=CC(C(NC(C(N(CCCCC)CCCCC)=O)CCC([O-])=O)=O)=C1.[Na]
分子式C22H31Cl2N2O4o Na
分子量481.4
溶解度≤1mg/ml in ethanol;1mg/ml in DMSO;1mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Lorglumide (sodium salt) is the first nonpeptidic, selective and potent inhibitor of the CCK-A receptor [1][2][3][4] .

Cholecystokinin (CCK) is a peptide hormone that plays important roles in the physiological regulation of pancreatic enzyme secretion, induction of pancreatic growth, smooth muscle contraction in the gall bladder and stomach, and modulation of feeding and behavior [1][2][3].

Lorglumide (CR1409) is the first nonpeptidic, selective and potent inhibitor of the CCK-A receptor. Lorglumide inhibited CCK A receptor and CCK B receptor with IC50 values of 50 nM and 3 μM, respectively [4]. In the guinea-pig isolated ileum, Lorglumide (0.06-2.1 μM) antagonized longitudinal muscle responses to ceruletide (a CCK-related decapeptide) and CCK-octapeptide (CCK-8) in a concentration dependent and competitive manner. Lorglumide (0.2-0.4 μM) also blocked contractions of the circular muscle induced by ceruletide [2].

In mice, CR1409 completely abolished the trophic effects of exogenous CCK and significantly inhibited the effects of chronic camostate feeding. CR1409 reduced pancreatic weight, DNA and protein content [3].

References:
[1].  Makovec F, Peris W, Revel L, et al. Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives. J Med Chem. 1992 Jan;35(1):28-38.
[2].  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 Pharmacol. 1987 Apr;90(4):753-61.
[3].  Niederau C, Liddle RA, Williams JA, et al. Pancreatic growth: interaction of exogenous cholecystokinin, a protease inhibitor, and a cholecystokinin receptor antagonist in mice. Gut. 1987;28 Suppl:63-9.
[4].  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. Br J Pharmacol. 1989 Mar;96(3):661-9.