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Lorglumide (sodium salt) Catalog No.GC10360

nonpeptidic antagonist of the CCK A receptor

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1021868-76-7 SDF
Chemical Name 4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxo-pentanoic acid, monosodium salt
Canonical SMILES ClC1=C(Cl)C=CC(C(NC(C(N(CCCCC)CCCCC)=O)CCC([O-])=O)=O)=C1.[Na]
Formula C22H31Cl2N2O4 • Na M.Wt 481.4
Solubility ≤1mg/ml in ethanol;1mg/ml in DMSO;1mg/ml in dimethyl formamide Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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].

[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.