2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Cholecystokinin Receptor
  5. CCKAR Isoform

CCKAR

The Cholecystokinin A receptor is a human protein, also known as CCKAR or CCK1. The CCK1R has high affinity for cholecystokinin (CCK) and related peptides that are sulfated on a tyrosine in the 7th position from the COOH terminus with a low affinity for gastrin. In humans, the results of numerous studies support a role for CCK1R in regulation of a variety of physiological processes including gallbladder contraction, sphincter of Oddi relaxation, stimulation of pancreatic secretion, inhibition of acid secretion, relaxation of lower esophageal sphincter tone, slowing of colonic motility and regulation of satiety.

CCKAR Related Products (7):

Cat. No. Product Name Effect Purity
  • HY-11077
    SR 146131
    		Agonist 98.81%
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
  • HY-P1096
    A71623
    		Agonist 99.90%
    A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively.
  • HY-101764
    Lintitript
    		Antagonist 99.58%
    Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.
  • HY-B2154
    Loxiglumide
    		Antagonist ≥98.0%
    Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
  • HY-123434
    PD-149164
    		Agonist
    PD-149164 is a potent agonist of cholecystokinin B (CCK-B) receptor, with IC50 values of 0.083 nM and 75 nM in binding assay to CCK-B and CCK-A.
  • HY-119127
    TP-680
    		Antagonist
    TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCKA receptors (IC50=1.2 nM) than to rat brain CCKB receptors (IC50=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases.
  • HY-129810
    PD 135158
    		Antagonist
    PD 135158 (CAM 1028) is a selective CCKB receptor antagonist with an IC50 of 2.8 nM against mouse cortex CCKB. PD 135158 shows anxiolytic activity.