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

Cholecystokinin Receptor

CCK Receptor

Cholecystokinin Receptor

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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 Isoform Specific Products:

Cholecystokinin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-105226B
    CI-988 hemihydrate
    		Antagonist ≥99.0%
    CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects.
    CI-988 hemihydrate
  • HY-P2677
    CCK (26-31) sulfated
    CCK (26-31) (sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety.
    CCK (26-31) sulfated
  • HY-P0196A
    Cholecystokinin Octapeptide, desulfated TFA
    Cholecystokinin Octapeptide, desulfated (CCK Octapeptide, desulfated) TFA is a synthetic desulfated Cholecystokinin octapeptide (HY-P0093).
    Cholecystokinin Octapeptide, desulfated 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-P1593A
    Mini Gastrin I, human TFA
    		98.13%
    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-P2932A
    Cholecystokinin-33 free acid
    Cholecystokinin-33 free acid is an analogue of Cholecystokinin (HY-P2932). C-terminal amidation is important for binding of Cholecystokinin to its receptors, and removing the amide group would decrease Cholecystokinin activity. Cholecystokinin-33 free acid can be used to study C-terminal amidation of Cholecystokinin-33.
    Cholecystokinin-33 free acid
  • HY-U00062
    Tarazepide
    		Antagonist
    Tarazepide is a potent and specific CCK-A receptor antagonist.
    Tarazepide
  • HY-125314
    AG-041R
    		Antagonist 99.9%
    AG-041R is a potent and selective CCK2 Receptor/Gastrin antagonist. AG-041R inhibits gastrin-evoked secretion of pancreastatin with an IC50 of 2.2 nM. AG-041R inhibits cell growth of Mastomys ECL carcinoid tumor cells.
    AG-041R
  • HY-A0261A
    Pentagastrin meglumine
    		Agonist
    Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor agonist with an EC50 value of 11 nM. 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-100481
    RP 72540
    		Antagonist
    RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors.
    RP 72540
  • HY-177507
    FE101120
    		Agonist
    FE101120 is a non-peptide agonist CCK2 receptor agonist. FE101120 can be used for the study of diabetes.
    FE101120
  • 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-117437
    Azintamide
    		Modulator
    Azintamide (Bilipurum) can be used for the research of psoriasis vulgaris, dyspepsia and other conditions.
    Azintamide
  • HY-114966
    RP73870
    		Antagonist
    RP73870 is an orally active gastrin/cholecystokinin-B receptor antagonist. RP73870 inhibits basal gastric acid secretion in the rat. RP73870 has potent anti-ulcer activity.
    RP73870
  • HY-118314
    CI-1015
    CI-1015 is a potent CCK-B receptor antagonist.
    CI-1015
  • HY-P2592
    Ro 23-7014
    Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7).
    Ro 23-7014
  • 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-11074
    CE-326597
    		Agonist
    CE-326597 is a small molecule agonist of the cholecystokinin A receptor (CCKAR). CE-326597 occupies only the lower half of the TMD pocket and cannot mimic the crucial interaction between CCK-8 and ECL1-3. CE-326597 can be used to study metabolic diseases and gastrointestinal dysfunction.
    CE-326597
  • HY-105226A
    CI-988 meglumin
    		Antagonist
    CI-988 meglumin is a cholecystokinin 2 receptor (CCK2R) antagonist. CI-988 meglumin prevents the gastrin-mediated protection of the heart with ischemia/reperfusion injury.
    CI-988 meglumin
Cholecystokinin Receptor Isoform Comparison

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