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

Cholecystokinin Receptor Antagonist

Cholecystokinin Receptor Antagonists (28):

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-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-118546
    JNJ-17156516
    		Antagonist
    JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist.
  • 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 Kis 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-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 99.74%
    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-17617
    Nastorazepide
    		Antagonist 99.95%
    Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  • HY-101764
    Lintitript
    		Antagonist 99.58%
    Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.
  • HY-B1439B
    Lorglumide sodium salt
    		Antagonist 99.71%
    Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.
  • HY-B2154
    Loxiglumide
    		Antagonist ≥98.0%
    Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
  • 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-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-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-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-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-148656
    PNB-001
    		Antagonist
    PNB-001 is an orally active CCK2 selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities.
  • HY-129810
    PD 135158
    		Antagonist
    PD 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.
  • HY-P2165
    N-acetyl CCK-(26-30) amide
    		Antagonist
    N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a cholecystokinin (CCK) receptor antagonist.
  • HY-U00363
    CHEMBL333994
    		Antagonist
    CHEMBL333994 is a potent and orally effective Cholecystokinin A (CCK-A) antagonist, with an IC50 of 0.67 nM.