2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Cholecystokinin Receptor
  5. Cholecystokinin Receptor Isoform
  6. Cholecystokinin Receptor Antagonist

Cholecystokinin Receptor Antagonist

Cholecystokinin Receptor Antagonists (46):

Cat. No. Product Name Effect Purity
  • HY-106301
    Devazepide
    		Antagonist 99.58%
    Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.
  • HY-14850
    Sograzepide
    		Antagonist 98.35%
    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. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
  • HY-100481
    RP 72540
    		Antagonist
    RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors.
  • HY-114966
    RP73870
    		Antagonist
    RP73870 is an orally active gastrin/cholecystokinin-B receptor antagonist. RP73870 inhibits basal gastric acid secretion in the rat. RP73870 has potent anti-ulcer activity.
  • HY-103354
    Proglumide sodium
    		Antagonist 99.85%
    Proglumide 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.
  • HY-B1330
    Proglumide
    		Antagonist 99.84%
    Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities.
  • HY-128878
    Dexloxiglumide
    		Antagonist 98.25%
    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).
  • HY-B1439B
    Lorglumide sodium salt
    		Antagonist 99.19%
    Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.
  • HY-106840A
    L-365260 hemihydrate
    		Antagonist 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.
  • HY-148656
    PNB-001
    		Antagonist 99.65%
    PNB-001 is an orally active CCK2 selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities.
  • HY-U00360
    (Rac)-Sograzepide
    		Antagonist 98.98%
    (Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
  • HY-105226B
    CI-988 hemihydrate
    		Antagonist
    CI-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.
  • HY-105257
    Pranazepide
    		Antagonist 99.81%
    Pranazepide (FR120480) is a cholecystokinin-A receptor antagonist.
  • HY-U00062
    Tarazepide
    		Antagonist
    Tarazepide is a potent and specific CCK-A receptor antagonist.
  • HY-150036
    Anthramycin
    		Antagonist
    Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice.
  • HY-120381
    PD 136450
    		Antagonist
    PD 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.
  • HY-103354A
    Proglumide hemicalcium
    		Antagonist
    Proglumide 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.
  • HY-118546
    JNJ-17156516
    		Antagonist
    JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist.
  • HY-169139
    Spiroglumide
    		Antagonist
    Spiroglumide (CR-2194) is a selective cholecystokinin B (CCKB) receptor antagonist.
  • HY-103357A
    LY262691
    		Antagonist
    LY262691 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.