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. 상품명 효과 Purity Chemical Structure
  • HY-N14304
    Asperlicin
    		Antagonist
    Asperlicin is a cholecystokinin antagonist found in Aspergillus alliaceus.
    Asperlicin
  • HY-U00360R
    (Rac)-Sograzepide (Standard)
    		Antagonist
    (Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
    (Rac)-Sograzepide (Standard)
  • HY-118665
    L-736380
    		Antagonist
    L-736380 is a high affinity CCK-B (cholecystokinin B receptor) receptor antagonist, with IC50 values of 0.054 nM and 400 nM for CCK-B and CCK-A, respectively. L-736380 dose-dependently inhibits gastric acid secretion in anesthetized rats (ID50, 0.064 mg/kg) and ex vivo binding of [125I]CCK-8S in BKTO mice brain membranes (ED50, 1.7 mg/kg).
    L-736380
  • HY-B1439BR
    Lorglumide sodium (Standard)
    		Antagonist
    Lorglumide sodium salt (Standard) is the analytical standard of Lorglumide sodium salt. This product is intended for research and analytical applications. Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.
    Lorglumide sodium (Standard)
  • HY-162070
    CCK antagonist 1
    		Antagonist 99.96%
    CCK antagonist 1 (compound 3d) is a CCK antagonist with IC50s of 1.1 μM and 4 μM for CCK1 and CCK2, respectively. CCK antagonist 1 can be used for research of cancer and mental disease.
    CCK antagonist 1
  • HY-19290
    S-0509
    		Antagonist
    S-0509 is a selective CCKB/gastrin receptor antagonist. S-0509 has a strong anti-secretion effect. S-0509 helps prevent the occurrence of duodenal ulcers.
    S-0509
  • HY-116576
    LY219057
    		Antagonist
    LY219057 is a potent antagonist of cholecystokinin octapeptide (CCK-8), with the ID50 of 287.5 nM.
    LY219057
  • HY-123182
    PD-140548
    		Antagonist
    PD-140548 is a selective cholecystokinin (CCKA) receptor antagonist. PD-140548 can be used in schizophrenia research.
    PD-140548
  • HY-17617R
    Nastorazepide (Standard)
    		Antagonist
    Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide (Standard)
  • HY-125314
    AG-041R
    		Antagonist
    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-106840R
    L-365260 (Standard)
    		Antagonist
    L-365260 (Standard) is the analytical standard of L-365260 (HY-106840). This product is intended for research and analytical applications. L-365260 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 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
    L-365260 (Standard)
  • HY-U00387
    CCK-A receptor inhibitor 1
    		Inhibitor
    CCK-A receptor inhibitor 1 is a cholecystokinin A (CCK-A) receptor inhibitor with a binging IC50 of 340 nM.
    CCK-A receptor inhibitor 1
  • HY-U00375
    Gastrin/CCK antagonist 1
    		Antagonist
    Gastrin/CCK antagonist 1 is an antagonist of gastrin/CCK, used for the research of gastrointestinal disorders.
    Gastrin/CCK antagonist 1
Cholecystokinin Receptor Isoform Comparison

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