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

Cholecystokinin Receptor

CCK Receptor

Cholecystokinin Receptor

Related Products

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Cholecystokinin receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin. Two types of functional membrane receptors, cholecystokinin A receptor (CCK-AR), located mainly on pancreatic acinar cells, and CCK-BR, mostly in the stomach and nervous system tissues, have been identified as the endogenous receptors of CCK. Both have high affinity for the sulfated CCK octapeptide (CCK-8), whereas only the CCK-BR has high affinity for gastrin.

CCK is a peptide hormone discovered in the small intestine. Together with secretin and gastrin, CCK constitutes the classical gut hormone triad. In addition to gallbladder contraction, CCK also regulates pancreatic enzyme secretion and growth, intestinal motility, satiety signalling and the inhibition of gastric acid secretion. CCK is also a transmitter in central and intestinal neurons.

Cholecystokinin Receptor Related Products (49):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B2154
    Loxiglumide
    		Antagonist ≥98.0%
    Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
    Loxiglumide
  • HY-128878
    Dexloxiglumide
    		Antagonist 98.25%
    Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).
    Dexloxiglumide
  • HY-106840A
    L-365260 hemihydrate
    		Antagonist 99.75%
    L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.
    L-365260 hemihydrate
  • HY-P1593A
    Mini Gastrin I, human TFA
    		99.09%
    Mini Gastrin I, human (TFA) is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
    Mini Gastrin I, human TFA
  • HY-129357
    CCK-B Receptor Antagonist 2
    		Inhibitor 98.84%
    CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC50 of 1.82 μM.
    CCK-B Receptor Antagonist 2
  • HY-U00360
    (Rac)-Sograzepide
    		Antagonist 98.98%
    (Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
    (Rac)-Sograzepide
  • HY-A0261A
    Pentagastrin meglumine
    		Agonist
    Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury..
    Pentagastrin meglumine
  • HY-19445
    Gastrazole
    		Antagonist
    Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer.
    Gastrazole
  • HY-150036
    Anthramycin
    		Antagonist
    Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice.
    Anthramycin
  • HY-P0093R
    Sincalide (Standard)
    Sincalide (Standard) is the analytical standard of Sincalide. This product is intended for research and analytical applications. Sincalide (Cholecystokinin octapeptide, CCK‐8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK. CCK‐8 can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. CCK‐8 can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK.
    Sincalide (Standard)
  • HY-P1593
    Mini Gastrin I, human
    Mini Gastrin I, human is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
    Mini Gastrin I, human
  • HY-160045
    AP1153 aptamer sodium
    		Chemical
    AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo.
    AP1153 aptamer sodium
  • HY-106301R
    Devazepide (Standard)
    		Antagonist
    Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.
    Devazepide (Standard)
  • HY-103354A
    Proglumide hemicalcium
    		Antagonist
    Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities.
    Proglumide hemicalcium
  • HY-11076
    GI 181771
    		Agonist
    GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
    GI 181771
  • HY-118546
    JNJ-17156516
    		Antagonist
    JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist.
    JNJ-17156516
  • 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.
    PD 135158
  • HY-P2165
    N-acetyl CCK-(26-30) amide
    		Antagonist
    N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a cholecystokinin (CCK) receptor antagonist.
    N-acetyl CCK-(26-30) amide
  • HY-U00363
    CHEMBL333994
    		Antagonist
    CHEMBL333994 is a potent and orally effective Cholecystokinin A (CCK-A) antagonist, with an IC50 of 0.67 nM.
    CHEMBL333994
  • HY-111313
    JNJ-26070109
    		Antagonist
    JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.
    JNJ-26070109