CHEMBL333994

CHEMBL333994 (FK-480) is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC50 of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis[1][2][3].

Product Specifications

CAS Number

[167820-10-2]

Product Name Alternative

FK-480

UNSPSC

12352005

Target

Cholecystokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/1H-Indole-2-carboxamide,_N--_3R_-1-_2-fluorophenyl_-3,4,6,7-tetrahydro-4-oxopyrrolo-3,2,1-jk--1,4-benzodiazepin-3-yl--.html

Solubility

10 mM in DMSO

Smiles

O=C(C(N1)=CC2=C1C=CC=C2)N[C@H]3C(N4C5=C(CC4)C=CC=C5C(C6=CC=CC=C6F)=N3)=O

Molecular Formula

C26H19FN4O2

Molecular Weight

438.45

References & Citations

[1]Satoh Y, et al. Studies on a novel, potent and orally effective cholecystokinin A antagonist, FK-480. Synthesis and structure-activity relationships of FK-480 and related compounds. Chem Pharm Bull (Tokyo) . 1994 Oct;42 (10) :2071-83.|[2]Funakoshi A, et al. Effect of a new cholecystokinin antagonist (FK 480) on gene expression of cholecystokinin and secretin in rat intestine. J Gastroenterol. 1994 Jun;29 (3) :385-7. |[3]Moriyoshi Y, et al. Duration of anti-cholecystokinin (CCK) action on the rat exocrine pancreas of new CCK receptor antagonist FK480 administered orally. J Gastroenterol. 1996 Apr;31 (2) :249-53