CCKBR

The cholecystokinin B receptor also known as CCKBR or CCK2R. CCK2R is a G protein-coupled receptor for gastrin and cholecystokinin (CCK), regulatory peptides of the brain and gastrointestinal tract. CCK2R has a high affinity for both gastrin and its COOH amidated analogues longer than the tetrapeptide, as well as cholecystokinin(CCK).CCK2R is found principally in the central nervous system and the gastrointestinal tract.

CCKBR Related Products (10):

By Type:	Selective (4)
By Effects:	Agonist (1) Antagonists (7) Activator (1)

Cat. No.	Product Name	Effect	Purity

HY-P1097

Gastrin I, human		99.93%
Gastrin I, human is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor.

HY-A0261

Pentagastrin	Activator	99.97%
Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCK_B) receptor antagonists with IC₅₀ values of 11 nM and 1100 nM for CCK_B and CCK_A, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury..

HY-106840

L-365260	Antagonist	99.93%
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is 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.

HY-19445

Gastrazole	Antagonist
Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer.

HY-155205

GV150013X	Antagonist
GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with K_i of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder.

HY-123434

PD-149164	Agonist
PD-149164 is a potent agonist of cholecystokinin B (CCK-B) receptor, with IC₅₀ values of 0.083 nM and 75 nM in binding assay to CCK-B and CCK-A.

HY-106347

Itriglumide	Antagonist
Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC₅₀ of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC₅₀ of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity.

HY-129810

PD 135158	Antagonist
PD 135158 (CAM 1028) is a selective CCK_B receptor antagonist with an IC₅₀ of 2.8 nM against mouse cortex CCK_B. PD 135158 shows anxiolytic activity.

HY-111313

JNJ-26070109	Antagonist
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pK_is 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.

HY-119127

TP-680	Antagonist
TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCK_A receptors (IC₅₀=1.2 nM) than to rat brain CCK_B receptors (IC₅₀=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases.

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