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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AP1153 aptamer sodium
0 ImagesCat. No.: HY-160045AP1153 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.
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A71378
0 ImagesCat. No.: HY-111918CAS No.: 127902-33-4A71378 is a selectivity CCK-A receptor agonist the IC50 values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC50 = 0.16 nM) and ileal muscle contraction (EC50 = 3.7 nM).
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Sut-8701
0 ImagesCat. No.: HY-129688CAS No.: 123577-73-1Sut-8701 is a Cholecystokinin (HY-P2932) analog that effectively slows the degenerative process of Alzheimer's disease by protecting the integrity of cholinergic neurons in the nucleus basalis.
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FE100726
0 ImagesCat. No.: HY-177506CAS No.: 158459-39-3FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.
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Gastrazole free acid
0 ImagesCat. No.: HY-106231CAS No.: 174610-98-1Synonyms: JB95008 free acidGastrazole (JB95008) free acid is a gastrin receptor antagonist with activity against pancreatic cancer.
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PD 136450
0 ImagesCat. No.: HY-120381CAS No.: 139067-52-0Synonyms: CAM 1189PD 136450 (CAM 1189) is an antagonist for cholecystokinin 2 (CCK2). PD 136450 exhibits anti-secretory, anxiolytic and anti-ulcer activities, inhibits gastric acid secretion (IC50=1 mg/kg), and ameliorates the haemorrhagic lesions (IC50=4.7 mg/kg) in rats.
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Minigastrin
0 ImagesCat. No.: HY-P5109CAS No.: 60748-07-4Minigastrin is an acidic peptide. Minigastrin can be used to study peptidepeptide interaction.
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Proglumide hemicalcium
0 ImagesCat. No.: HY-103354ACAS No.: 85068-56-0Proglumide 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.
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GI 181771
0 ImagesCat. No.: HY-11076CAS No.: 305366-98-7GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
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CLIK-148
0 ImagesCat. No.: HY-164634CAS No.: 215098-90-1CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.
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PF-04756956
0 ImagesCat. No.: HY-117828CAS No.: 1228934-52-8PF-04756956 is a highly potent type 1 cholecystokinin receptor (CCK1R) agonist (EC50=0.47 nM). PF-04756956 is promising for research of obesity and related metabolic disorders.
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JNJ-17156516
0 ImagesCat. No.: HY-118546CAS No.: 649551-06-4JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist.
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Spiroglumide
0 ImagesCat. No.: HY-169139CAS No.: 137795-35-8Synonyms: CR-2194Spiroglumide (CR-2194) is a selective cholecystokinin B (CCKB) receptor antagonist.
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Ceclazepide
0 ImagesCat. No.: HY-109028CAS No.: 1801749-44-9Synonyms: TR2-ACeclazepide (TR2-A), a CCK2R antagonist, is an orally active Mycobacterium abscessus inhibitor. Ceclazepide inhibits acid secretion in rats. Ceclazepide effectively suppresses the growth of M. abscessus wild-type strain and multiple subspecies. Ceclazepide inhibits M. abscessus growth within macrophages without causing harm.
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GW-5823
0 ImagesCat. No.: HY-117781CAS No.: 1356689-41-2GW-5823 is a selective CCK-AR agonist with an EC50 of 70 nM. GW-5823 can be studied in research on obesity.
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ARL 15849XX
0 ImagesCat. No.: HY-P1710CAS No.: 152548-39-5ARL 15849XX is a cholecystokinin-8 (CCK-8) analog.
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Nastorazepide hemicalcium
0 ImagesCat. No.: HY-14575CAS No.: 343326-69-2Synonyms: Z-360 hemicalciumNastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
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Caerulein acetate
0 ImagesCat. No.: HY-158722CAS No.: 2760881-68-1Caerulein acetate is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide acetate is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.
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PD 135158
0 ImagesCat. No.: HY-129810CAS No.: 130325-35-8Synonyms: CAM 1028PD 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.
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LY262691
0 ImagesCat. No.: HY-103357ACAS No.: 138932-35-1LY262691 is a selective CCK-B antagonist with antipsychotic properties. LY262691 decreases the number of spontaneously active A9 and A10 dopamine cells and can be utilized in antipsychotic research.
