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gastrin receptor

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55

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21

Peptides

4

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Products

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1097
    Gastrin I, human
    Maximum Cited Publications
    17 Publications Verification

    		 Cholecystokinin Receptor Endocrinology
    Gastrin I, human is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor.
    Gastrin I, human
  • HY-P2671
    [Leu15]-Gastrin I (human)

    		Cholecystokinin Receptor Cancer
    [Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
    [Leu15]-Gastrin I (human)
  • HY-P0195
    Bombesin
    1 Publications Verification

    		 Bombesin Receptor Neurological Disease Metabolic Disease
    Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors .
    Bombesin
  • HY-14850
    Sograzepide
    1 Publications Verification

    Netazepide; YF 476; YM-220

    		 Cholecystokinin Receptor Metabolic Disease Endocrinology
    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 .
    Sograzepide
  • HY-103286
    PD176252
    2 Publications Verification

    		 Bombesin Receptor Cancer
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
    PD176252
  • HY-17617
    Nastorazepide

    Z-360

    		 Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt Neurological Disease Cancer
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
    Nastorazepide
  • HY-106840
    L-365260
    2 Publications Verification

    		 Cholecystokinin Receptor Neurological Disease Metabolic Disease
    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 .
    L-365260
  • HY-P0107A
    RC-3095 TFA
    1 Publications Verification

    		 Bombesin Receptor Inflammation/Immunology
    RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
    RC-3095 TFA
  • HY-125556
    Tetragastrin
    1 Publications Verification

    Cholecystokinin tetrapeptide; CCK-4

    		 Cholecystokinin Receptor Metabolic Disease
    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 .
    Tetragastrin
  • HY-N2600
    Kuwanon H

    		Bombesin Receptor Cancer
    Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
    Kuwanon H
  • HY-116216
    PD 168368

    		Bombesin Receptor Cancer
    PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM . PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist . PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively .
    PD 168368
  • HY-103355
    YM022
    2 Publications Verification

    		 CCR Metabolic Disease
    YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .
    YM022
  • HY-P1423A
    BA 1 TFA

    		Bombesin Receptor Metabolic Disease Cancer
    BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM .
    BA 1 TFA
  • HY-103281
    Litorin

    		Bombesin Receptor Metabolic Disease
    Litorin, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. Litorin stimulates the contraction of smooth muscle, stimulates gastrin, gastric acid, and pancreatic secretion, and suppresses the nutriment in vivo .
    Litorin
  • HY-P0107
    RC-3095
    1 Publications Verification

    		 Bombesin Receptor Inflammation/Immunology
    RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
    RC-3095
  • HY-P0039
    BIM-26226

    		Bombesin Receptor Cancer
    BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth .
    BIM-26226
  • HY-P10896
    NOTA-P2-RM26

    		Bombesin Receptor Cancer
    NOTA-P2-RM26 is an antagonist of Bombesin (HY-P0195) analogs, and the gastrin-releasing peptide receptor (GRPR/BB2) is a molecular target for prostate cancer visualization. NOTA-P2-RM26 is labeled with 111In and 68Ga for prostate cancer imaging studies using PET and SPECT/CT .
    NOTA-P2-RM26
  • HY-W343750
    [Tyr4]-Bombesin

    		Bombesin Receptor Metabolic Disease
    [Tyr4]-Bombesin is a Bombesin analogue, is a ligand of gastrin-releasing peptide receptor (GRPR) .
    [Tyr4]-Bombesin
  • HY-103277A
    BIM 23042 TFA
    1 Publications Verification

    		 Bombesin Receptor Neurological Disease Metabolic Disease
    BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
    BIM 23042 TFA
  • HY-103277
    BIM 23042

    		Bombesin Receptor Neurological Disease Metabolic Disease
    BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release .
    BIM 23042
  • HY-P5413
    [Lys3]-Bombesin

    		Cholecystokinin Receptor Others
    [Lys3]-Bombesin is a biological active peptide. (PET (Positron Emission Tomography) imaging of [Lys3]-bombesin is able to detect gastrin-releasing peptide receptor (GRPR) positive prostate cancer. An immunoconjugate of [Lys3]-bombesin and corresponding monoclonal antibody can specifically induce (CD64)-dependent monocyte and neutrophil-mediated lysis of small cell carcinoma.)
    [Lys3]-Bombesin
  • HY-115974
    GRPR antagonist-1

    		Bombesin Receptor Cancer
    GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity .
    GRPR antagonist-1
  • HY-P11352
    JMV594

    RM26

    		 Bombesin Receptor Cancer
    JMV594 (Compound RM 26) is a bombesin analogue with high affinity and antagonistic effect for gastrin releasing peptide receptor (GRPR).JMV594 can be used for the research of cancer, such as Prostate cancer .
    JMV594
  • HY-106840A
    L-365260 hemihydrate
    2 Publications Verification

    		 Cholecystokinin Receptor Neurological Disease Metabolic Disease
    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 .
    L-365260 hemihydrate
  • HY-125314
    AG-041R

    		Cholecystokinin Receptor Endocrinology Cancer
    AG-041R is a potent and selective CCK2 Receptor/Gastrin antagonist. AG-041R inhibits gastrin-evoked secretion of pancreastatin with an IC50 of 2.2 nM. AG-041R inhibits cell growth of Mastomys ECL carcinoid tumor cells .
    AG-041R
  • HY-106347
    Itriglumide

    CR 2945

    		 Cholecystokinin Receptor Inflammation/Immunology
    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 .
    Itriglumide
  • HY-P5520
    GB-6

    		Bombesin Receptor Radionuclide-Drug Conjugates (RDCs) Cancer
    GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
    GB-6
  • HY-129357
    CCK-B Receptor Antagonist 2

    		Cholecystokinin Receptor Metabolic Disease
    CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC50 of 1.82 μM .
    CCK-B Receptor Antagonist 2
  • HY-155205
    GV150013X

    		Cholecystokinin Receptor Neurological Disease
    GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder .
    GV150013X
  • HY-121278
    Benzotript

    Benzotriptum

    		 Cholecystokinin Receptor Inflammation/Immunology Cancer
    Benzotript (Benzotriptum) is a cholecystokinin-receptor (CCK) and gastrin receptor antagonist. Benzotript shows antiproliferative effects in human colon carcinoma cell lines .
    Benzotript
  • HY-176150
    AMTG-DA1

    		Bombesin Receptor Cancer
    AMTG-DA1 is a Gastrin-releasing peptide receptor (GRPR) ligand. AMTG-DA1 can be used in the study of cancer .
    AMTG-DA1
  • HY-P1423
    BA 1

    		Bombesin Receptor Metabolic Disease Cancer
    BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM .
    BA 1
  • HY-19290
    S-0509

    		Cholecystokinin Receptor Others
    S-0509 is a selective CCKB/gastrin receptor antagonist. S-0509 has a strong anti-secretion effect. S-0509 helps prevent the occurrence of duodenal ulcers .
    S-0509
  • HY-111918
    A71378

    		Cholecystokinin Receptor Metabolic Disease
    A71378 is a selectivity CCK-A receptor agonist the IC50 values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC50 = 0.16 nM) and ileal muscle contraction (EC50 = 3.7 nM) .
    A71378
  • HY-124517
    Burimamide

    		Histamine Receptor Adrenergic Receptor Neurological Disease Inflammation/Immunology
    Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768) .
    Burimamide
  • HY-19445
    Gastrazole

    JB95008

    		 Cholecystokinin Receptor Cancer
    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 .
    Gastrazole
  • HY-106231
    Gastrazole free acid

    JB95008 free acid

    		 Cholecystokinin Receptor Others
    Gastrazole (JB95008) free acid is a gastrin receptor antagonist with activity against pancreatic cancer.
    Gastrazole free acid
  • HY-120302
    PD 140376

    		Cholecystokinin Receptor Metabolic Disease
    PD 140376 is a potent antagonist for the cholecystokininB/gastrin receptor, with Ki values of 0.18 nM and 0.21 nM in guinea-pig cortex and gastric gland membranes, respectively .
    PD 140376
  • HY-114966
    RP73870

    		Cholecystokinin Receptor Inflammation/Immunology
    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 .
    RP73870
  • HY-P0221B
    PACAP (1-38) free acid TFA

    		PACAP Receptor Endocrinology
    PACAP (1-38) free acid TFA is an endogenous neuropeptide. PACAP (1-38) free acid TFA potently stimulates antral motility and somatostatin secretion, inhibits the secretion of gastrin and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide and substance P. PACAP (1-38) free acid TFA also enhances N-methyl-D-aspartate receptor function and expression of brain-derived neurotrophic factor through RACK1 .
    PACAP (1-38) free acid TFA
  • HY-115975
    GRPR antagonist-2

    		Bombesin Receptor Cancer
    GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity .
    GRPR antagonist-2
  • HY-N2600R
    Kuwanon H (Standard)

    		Reference Standards Bombesin Receptor Cancer
    Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .
    Kuwanon H (Standard)
  • HY-129516
    A-70874

    		Cholecystokinin Receptor Metabolic Disease
    A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (30-33) (CCK-4). A-70874 is an agonist that stimulates pancreatic amylase release and a partial agonist that stimulates pancreatic phosphoinositide decomposition. A-70874 has an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor. Cholecystokinin (CCK) receptors are divided into CCK-A (digestive tract) and CCK-B (brain). A-70874 has an affinity of 1.6 μM for the CCK-B/gastrin receptor .
    A-70874
  • HY-P2055
    A-57696

    		Endogenous Metabolite Endocrinology
    A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
    A-57696
  • HY-125431
    LY 202769

    		Cholecystokinin Receptor Neurological Disease Metabolic Disease
    LY 202769 (Example 26) is a cholecystokinin (CCK) and gastrin receptor (gastrin receptor) antagonist. LY 202769 is applicable for the research of gastrointestinal diseases and central nervous system diseases .
    LY 202769
  • HY-14575
    Nastorazepide hemicalcium

    Z-360 hemicalcium

    		 Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt Neurological Disease Cancer
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain .
    Nastorazepide hemicalcium
  • HY-17617R
    Nastorazepide (Standard)

    Z-360 (Standard)

    		 Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt Reference Standards Neurological Disease Cancer
    Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
    Nastorazepide (Standard)
  • HY-105226A
    CI-988 meglumin

    PD134308 meglumin

    		 Cholecystokinin Receptor Cardiovascular Disease
    CI-988 meglumin is a cholecystokinin 2 receptor (CCK2R) antagonist. CI-988 meglumin prevents the gastrin-mediated protection of the heart with ischemia/reperfusion injury .
    CI-988 meglumin
  • HY-116260
    RP-69758

    		Cholecystokinin Receptor Neurological Disease Inflammation/Immunology
    RP-69758 is a potent and selective non-peptide cholecystokinin-B (CCKB)/gastrin receptor antagonist. RP-69758 exhibits >200-fold selectivity for CCKB over CCKA receptors. RP-69758 antagonizes CCK-8-induced neuronal firing in rat hippocampal slices. RP-69758 inhibits Pentagastrin (HY-A0261)-induced gastric acid secretion in the rat. RP-69758 can be used for neurological disorders and gastrointestinal disease research .
    RP-69758
  • HY-103355R
    YM022 (Standard)

    		Reference Standards CCR Metabolic Disease
    YM022 (Standard) is the analytical standard of YM022 (HY-103355). This product is intended for research and analytical applications. YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .
    YM022 (Standard)

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