Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Cholecystokinin receptors (CCKRs) are a class of G-protein coupled receptors that respond to the peptide hormone cholecystokinin (CCK). CCK is predominantly found in the gastrointestinal tract and the central nervous system. There are two primary subtypes of cholecystokinin receptors: CCK-A (CCK1) receptor, mainly located in the pancreas, gallbladder, stomach, and certain areas of the brain, and CCK-B (CCK2) receptor, found predominantly in the brain and the stomach lining.
The primary function of CCKRs is to mediate the physiological actions of CCK. In the digestive system, CCK is involved in stimulating the digestion of fats and protein. It achieves this by inducing the secretion of digestive enzymes from the pancreas and bile from the gallbladder. Moreover, CCK plays a crucial role in regulating appetite by promoting satiety, making it a point of interest in obesity research.
In the central nervous system, CCK is involved in various functions, including anxiety, pain, and neuroendocrine control. CCK and its receptors are also implicated in psychiatric disorders like anxiety and panic attacks.
CCKRs are also significant in the medical field as potential targets for therapeutic intervention. For instance, CCK-B antagonists are being explored for their potential in treating anxiety disorders and gastrointestinal issues.
Overall, cholecystokinin receptors are integral to various physiological processes, from digestion to brain function, highlighting their importance in both understanding bodily functions and developing medical treatments.
Synonyms: Caerulein; Cerulein; FI-6934
Ceruletide is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.
SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
Synonyms: Cholecystokinin tetrapeptide; CCK-4
Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion. Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist. Gastric mucosal protection.
CCKBR agonist-1 is a potent agonist of the cholecystokinin B receptor (CCKBR), preferentially activating Gq-proteins with an EC50 of 35 pM. This compound enhances neuronal survival, demonstrated by an EC50 of 37 pM, and has shown efficacy in mitigating cognitive decline in murine models. Mechanistically, CCKBR agonist-1 upregulates α-secretase (ADAM10) and the calcium signaling molecule PLCB4, leading to decreased amyloid β (Aβ) plaque formation and enhancement of long-term potentiation (LTP). CCKBR agonist-1 serves as a valuable tool for research into Alzheimer's disease.
CCKBR agonist-2 is a selective agonist for the cholecystokinin B receptor (CCKBR), primarily activating the Gi signaling pathway with an EC50 of 0.27 nM. This compound demonstrates minimal interaction with Gq and Gs pathways, making it a valuable tool for studying Gi-mediated cellular responses. Despite its potency in activating CCKBR-Gi signaling, CCKBR agonist-2 does not exhibit significant neuroprotective effects in mouse models of Alzheimer's disease, highlighting the complexity of cognitive function modulation. This reagent is useful in research exploring the roles of CCKBR signaling in various physiological and pathological contexts.
A71623 is a potent and highly selective full agonist for the CCK-A receptor, demonstrating a strong affinity with an IC50 of 3.7 nM in guinea pig pancreatic tissues and minimal activity at CCK-B receptors with an IC50 of 4500 nM. Its selectivity makes A71623 a valuable tool for studying CCK-A receptor functions and related physiological processes. This compound is applicable in research exploring gastrointestinal physiology, neurobiology, and the modulation of satiety signaling pathways.
CE-326597 is a small molecule agonist of the cholecystokinin A receptor (CCKAR). It selectively engages the lower region of the transmembrane domain pocket, offering unique insights into receptor activation that differ from the natural ligand CCK-8. This compound is valuable for studying metabolic disorders and gastrointestinal dysfunction, enabling researchers to explore the therapeutic potential of CCKAR modulation.
A71378 is a selective CCK-A receptor agonist with an IC50 of 0.4 nM for the pancreatic CCK-A receptor, and significantly higher IC50 values for the cortical CCK-B and gastrin receptors at 300 nM and 1,200 nM, respectively. This compound effectively stimulates pancreatic amylase secretion with an EC50 of 0.16 nM and induces ileal muscle contraction with an EC50 of 3.7 nM. A71378 is valuable for research applications focusing on gastrointestinal pharmacology and the role of CCK-A receptors in digestive processes.
FE100726 is a potent Cholecystokinin 2 (CCK2) receptor agonist, exhibiting high binding affinity to the CCK2 receptor. This compound has been demonstrated to effectively stimulate gastric acid secretion in anesthetized rat models. FE100726 is valuable for research related to diabetes and gastrointestinal physiology, offering insights into the role of CCK2 signaling pathways.
Out of stock
All 3 sizes
PF-04756956 is a potent agonist of the type 1 cholecystokinin receptor (CCK1R) with an EC50 of 0.47 nM. This compound is valuable for studying the mechanisms underlying obesity and associated metabolic disorders. Its activity at CCK1R makes it a significant tool for investigating therapeutic strategies aimed at regulating appetite and metabolic function.
Out of stock
All 3 sizes
ARL 15849XX is a potent agonist of the cholecystokinin receptor, specifically designed as an analog of cholecystokinin-8 (CCK-8). It effectively engages CCK receptors, stimulating pathways associated with gastrointestinal functions and satiety. This compound is valuable in research applications focusing on digestive physiology and neuropeptide signaling pathways.
Caerulein acetate is a decapeptide that functions as a potent agonist of the cholecystokinin receptor. It exhibits significant cholecystokinetic activity, promoting contraction of the gallbladder and facilitating bile duct function. This compound is widely used in research applications related to gastrointestinal motility and the study of digestive processes.
Out of stock
All 3 sizes
JMV 176 is a cholecystokinin (CCK) receptor agonist that exhibits its primary activity upon initial administration. Following a period of 3–4 hours, it transitions to function as a CCK antagonist. This dual-action characteristic makes JMV 176 valuable for research exploring CCK-related physiological processes and potential therapeutic applications in gastrointestinal disorders.
U-67827E is a cholecystokinin (CCK) agonist that modulates food intake by impacting gastrointestinal motility. This compound influences the latency to food consumption, potentially through the inhibition of gastric emptying and enhancement of gastric distention signaling. U-67827E is valuable for research applications investigating appetite regulation and the mechanisms of satiety.
JMV 170 is a selective CCK-B agonist that specifically targets the CCK-B receptor with a binding affinity ten times greater than that for the CCK-A receptor. This compound induces contractile effects in pig smooth muscle cells, exhibiting an EC50 value of 9 pmol/L. JMV 170 is primarily utilized in research applications focusing on gastrointestinal physiology and neurobiology, particularly in studies investigating the roles of cholecystokinin in smooth muscle contractility.
Out of stock
All 3 sizes
PD-149164 is a selective agonist of the cholecystokinin B (CCK-B) receptor, exhibiting high binding affinity with IC50 values of 0.083 nM for CCK-B and 75 nM for CCK-A. This compound is instrumental in studying the role of CCK-B receptors in physiological and pathological processes, including appetite regulation, anxiety, and enhanced memory function. It serves as a valuable tool for research in neuropharmacology and gastrointestinal studies.
Out of stock
All 3 sizes
A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (CCK-4), acting as an agonist for pancreatic amylase release. It also serves as a partial agonist, promoting phosphoinositide decomposition in pancreatic cells. With an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor, A-70874 shows a notable affinity of 1.6 μM for the CCK-B/gastrin receptor. This compound is valuable for investigating the physiological roles of CCK receptors in both the digestive system and the central nervous system.
GW-5823 is a selective agonist of the cholecystokinin A receptor (CCK-AR), exhibiting an EC50 of 70 nM. This compound plays a crucial role in modulating appetite and satiety signals, making it valuable for research focused on obesity and metabolic disorders. Its specificity allows for detailed investigations into CCK-AR-related pathways and therapeutic potentials in weight management.
