A selective antagonist of CCK1
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Product Type

Small Molecule Modulators
Receptor Pharmacology
Antagonists

Research Area

Lorglumide (sodium salt)

Item No. 17555

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxo-pentanoic acid, monosodium salt
CAS Number
1021868-76-7
Molecular Formula
C22H31Cl2N2O4 • Na
Formula Weight
481.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
SMILES
ClC1=C(Cl)C=CC(C(NC(C(N(CCCCC)CCCCC)=O)CCC([O-])=O)=O)=C1.[Na]
InChi Code
InChI=1S/C22H32Cl2N2O4.Na/c1-3-5-7-13-26(14-8-6-4-2)22(30)19(11-12-20(27)28)25-21(29)16-9-10-17(23)18(24)15-16;/h9-10,15,19H,3-8,11-14H2,1-2H3,(H,25,29)(H,27,28);/p-1
InChi Key
IEGKIAKFIRAEMH-UHFFFAOYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $36

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    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).1 It blocks CCK-mediated gut muscle contraction, pancreatic growth, and pancreatic secretion.2,3,4 Lorglumide is commonly used to study the roles of CCK1 in tissues and in animals.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. 35(1), 28-38 (1992).

    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. 90, 753-761 (1987).

    3. 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).

    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. 96, 661-669 (1989).

    5. Gamble, J., Kenny, S., and Dockray, G.J. Plasminogen activator inhibitor (PAI)-1 suppresses inhibition of gastric emptying by cholecystokinin (CCK) in mice. Regul. Pept. 185, 9-13 (2013).

    6. 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).