Dexloxiglumide

Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8) . Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors[1][2][3].

Product Specifications

CAS Number

[119817-90-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Cholecystokinin Receptor; P-glycoprotein

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/dexloxiglumide.html

Concentration

10mM

Purity

98.25

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(O)CC[C@@H](NC(C1=CC=C(Cl)C(Cl)=C1)=O)C(N(CCCOC)CCCCC)=O

Molecular Formula

C21H30Cl2N2O5

Molecular Weight

461.38

Precautions

H302, H315, H319, H335

References & Citations

[1]Scarpignato C, et al. Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10 (3) :411-9.|[2]Maselli MA, et al. CCK1 receptor antagonist, dexloxiglumide: effects on human isolated gallbladder. Potential clinical applications. Minerva Gastroenterol Dietol. 2003 Sep;49 (3) :211-6.|[3]Tolle-Sander, S., et al., (2003) . Characterization of dexloxiglumide in vitro biopharmaceutical properties and active transport. Journal of pharmaceutical sciences, 92 (10), 1968–1980.