Cholecystokinin Receptor
CCK Receptor
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
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Cholecystokinin Receptor Inhibitors
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Cholecystokinin Receptor Agonists
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Cholecystokinin Receptor Antagonists
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Cholecystokinin Receptor Activators
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Cholecystokinin Receptor Modulator
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Cholecystokinin Receptor Chemical
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Cholecystokinin Receptor Controls
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Cholecystokinin Receptor Related Products (136)
Related Products (136)
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Cholecystokinin Receptor Isoform Comparison
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Biotin-Gastrin-1, human (1-17)
0 ImagesBiotin-Gastrin-1, human (1-17) is a biological active peptide. (Biotin-labeled HY-P1097)
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Proglumide sodium
0 ImagesProglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
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Lintitript
0 ImagesSynonyms: SR 27897Lintitript (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.
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Nastorazepide
0 ImagesSynonyms: Z-360Nastorazepide (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.
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Loxiglumide
0 ImagesSynonyms: CR-1505Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
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CCKBR agonist-1
0 ImagesCCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC50 of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC50 of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease.
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T-0632
0 ImagesT-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
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Pranazepide
0 ImagesSynonyms: FR120480Pranazepide (FR120480) is a selective cholecystokinin-1 receptor (CCK1-R) antagonist with an IC50 of 0.67 nM against CCK1-R. Pranazepide is applicable for the research of pancreatic diseases.
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JNJ-26070109
0 ImagesJNJ-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.
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LY 225910
0 ImagesLY 225910 is a selective antagonist for cholecystokinin receptor (CCK2 receptor), which affects the excitatory response to morphine, and leads to morphine sensitization.
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PNB-001
0 ImagesPNB-001 is an orally active CCK2 selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities.
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Big Gastrin I (human) TFA
0 ImagesCat. No.: HY-P3446ABig Gastrin I, human (TFA) is a gastrointestinal hormone consisting of 34 amino acids. Big Gastrin I, human (TFA) can be used as a potential substance for the study of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurological diseases or cardiovascular diseases.
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L-365260 hemihydrate
0 ImagesCat. No.: HY-106840APurity: 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.
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A-65186
0 ImagesA-65186 is a CCK-A receptor antagonist with the activity of inhibiting CCK8-induced amylase secretion. A-65186 has high binding affinity for pancreatic CCK-A receptors, is more than 500 times more selective for CCK-A receptors than for CCK-B receptors, and can inhibit CCK8-induced amylase secretion.
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(Rac)-Sograzepide
0 ImagesSynonyms: (Rac)-Netazepide; (Rac)-YF 476; (Rac)-YM-220(Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
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GV150013X
0 ImagesGV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder.
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CCKBR agonist-2
0 ImagesCCKBR agonist-2 (Compound z-44) is a Gi-preferring CCKBR agonist. CCKBR agonist-2 effectively activates the CCKBR-Gi signaling pathway (EC50 = 0.27 nM), but has almost no activity on Gq and Gs signaling pathways. CCKBR agonist-2 shows no significant protective effect in the mouse Alzheimer's disease model, proving that the simple activation of the Gi signal pathway does not play a dominant role in the improvement of cognitive function.
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[Lys3]-Bombesin
![[Lys3]-Bombesin](https://file.medchemexpress.com/product_pic/hy-p5413.gif "Click to View [Lys3]-Bombesin Product Detail")
0 Images[Lys3]-Bombesin is a biological active peptide. (PET (Positron Emission Tomography) imaging of [Lys3]-bombesin is able to detect gastrin-releasing peptide receptor (GRPR) positive prostate cancer. An immunoconjugate of [Lys3]-bombesin and corresponding monoclonal antibody can specifically induce (CD64)-dependent monocyte and neutrophil-mediated lysis of small cell carcinoma.)
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CI-988 hemihydrate
0 ImagesCat. No.: HY-105226BSynonyms: PD134308 hemihydrateCI-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.
