- Cat. No.
- A11769
Loxiglumide (CR1505)
Synonyms: anoicacid; CR1505
Loxiglumide (CR1505) is a cholecystokinin antagonist
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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: anoicacid; CR1505
Loxiglumide (CR1505) is a cholecystokinin antagonist
Synonyms: Z360
Z-360 is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. It inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini.
Synonyms: Z360
Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
Synonyms: W 5219; CR 242
Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. IProglumide is a known cholecystokinin (CCK) antagonist.
Synonyms: CCK-8; CCK-8S; Kinevac
Sincalide, also known as CCK-8, is a drug used to treat cholecystitis. Sincalide is an octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.
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.
CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
Synonyms: CR-2017
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).
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: Netazepide; YF 476; YM-220
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM.
Gastrin I, human is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor.
[Leu15]-Gastrin I (human) is a peptide. Gastrin exerts its function through G-protein-coupled receptor called the cholecystokinin (CCK) or CCK-B receptor (CCK-BR).
Synonyms: CCK Octapeptide; desulfated
Cholecystokinin Octapeptide, desulfated is a synthetic desulfated octapeptides of cholecystokinin (CCK).
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.
Synonyms: CCK-(26-30) (sulfated)
N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a cholecystokinin (CCK) receptor antagonist.
CCK (26-31) (non-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) is also less active in non-sulfated than in sulfated form.
Synonyms: Cholecystokinin octapeptide ammonium; CCK-8 ammonium; SQ19844 ammonium
Sincalide ammonium is an amino acid polypeptide hormone analogue of cholecystokinin (CCK) that primarily targets gallbladder function. It is utilized in clinical settings for its ability to promote gallbladder contraction, thus facilitating the diagnosis of gallbladder and pancreatic disorders. By increasing bile secretion and causing the contraction of the gallbladder while relaxing the sphincter of Oddi, Sincalide ammonium aids in the efficient drainage of bile into the duodenum, making it a valuable tool in postevacuation cholecystography.
Antibacterial agent 241 is a histidine kinase (HK) inhibitor with IC50 values of 14 μM for CckA and 238 μM for PhoQ. It demonstrates moderate antibacterial activity against various bacterial strains, including E. coli DC2, Bacillus cereus, and Bacillus subtilis, with minimum inhibitory concentration (MIC) values ranging from 12 to 74 μg/mL. This compound is suitable for research applications targeting bacterial signaling pathways and antibiotic resistance mechanisms.
Synonyms: TR2-A
Ceclazepide is a cholecystokinin-2 receptor (CCK2R) antagonist that serves as an orally active inhibitor of Mycobacterium abscessus. This compound effectively reduces acid secretion in rat models and demonstrates significant suppression of both wild-type and multiple subspecies of M. abscessus. Importantly, Ceclazepide inhibits the growth of M. abscessus within macrophages while maintaining cell integrity, making it a valuable tool for research into mycobacterial infections and related therapeutic strategies.
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YM022 is a highly potent and selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor (CCK-BR). With Ki values of 68 pM for CCK-B and 63 nM for CCK-A, YM022 effectively blocks gastrin-induced gastric acid secretion and inhibits histidine decarboxylase activation in vivo. This compound is valuable for research applications related to gastrointestinal disorders and receptor signaling pathways.
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.
Synonyms: L-364,718; MK-329
Devazepide is a potent, competitive, and selective antagonist of the cholecystokinin (CCK) receptor. It exhibits high affinity with IC50 values of 81 pM, 45 pM, and 245 nM for rat pancreatic, bovine gallbladder, and guinea pig brain CCK receptors, respectively. This nonpeptide agent is primarily utilized in research focused on gastrointestinal disorders, providing insights into gastrointestinal physiology and the therapeutic potential of CCK receptor modulation.