Catalog No.
Product Name
Application
Product Information
Citations
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CKK Antagonist
JMV 179 is a cholecystokinin receptor (CKK) antagonist with an IC50 of 30 nM. This peptide analog is designed to inhibit CCK receptor activity, making it a valuable tool for studying the physiological and pathophysiological roles of CCK signaling. JMV 179 is utilized in various research applications, particularly in gastrointestinal studies and neuropharmacology, to explore the therapeutic potential of modulating CCK pathways. -
CCK B Inhibitor
PD-135666 is a potent dipeptide inhibitor of cholecystokinin B (CCK B) receptors, demonstrating an IC50 of 0.1 nM in mouse cerebral cortex. Unlike its enantiomer, PD-140548, which selectively targets CCK A receptors in rat pancreas, PD-135666 primarily interacts with CCK B receptors. This compound has been shown to exhibit anxiolytic effects in various animal models, making it a valuable tool for studying anxiety-related disorders and CCK receptor biology. -
CCK Fragment
Cholecystokinin-33 (swine) is a biologically active fragment of cholecystokinin (CCK) that primarily targets CCK receptors. It is known to reduce food intake and promote gallbladder contraction, making it relevant for studies focused on appetite regulation and gastrointestinal motility. This peptide can be utilized in research to investigate its roles in digestive processes and related metabolic disorders. -
CCK-A Receptor Antagonist
(rac)-CHEMBL333994 is a potent Cholecystokinin A (CCK-A) receptor antagonist with an IC50 of 0.67 nM, demonstrating effective oral bioavailability. This compound selectively targets peripheral CCK receptors, making it valuable for studying mechanistic pathways involved in gastrointestinal disorders. Its ability to increase CCK mRNA levels positions (rac)-CHEMBL333994 as a useful tool in research aimed at understanding chronic pancreatitis and related conditions. -
CCK-B Agonist
JMV 170 is a selective CCK-B agonist that specifically targets the CCK-B receptor with a binding affinity ten times greater than that for the CCK-A receptor. This compound induces contractile effects in pig smooth muscle cells, exhibiting an EC50 value of 9 pmol/L. JMV 170 is primarily utilized in research applications focusing on gastrointestinal physiology and neurobiology, particularly in studies investigating the roles of cholecystokinin in smooth muscle contractility. -
CCK-B Receptor Antagonist
DA-3934 is a cholecystokinin (CCK)-B receptor antagonist that effectively inhibits gastric acid secretion. Through its mechanism of action, DA-3934 blocks Pentagastrin-induced gastric acid release in rat models. This compound is valuable for research applications focused on gastrointestinal physiology and the modulation of acid secretion pathways. -
CCK1 Antagonist
VL-0395 is a selective antagonist of the cholecystokinin receptor 1 (CCK1), demonstrating an IC50 of 0.197 μM in rat pancreatic acinar cells. This compound effectively inhibits CCK1-mediated signaling pathways, making it a valuable tool for studying the physiological and pathological roles of CCK1 in digestive processes and pancreatic function. Its specificity and potency position VL-0395 as an essential reagent for research in gastrointestinal pharmacology and related fields. -
CCK Receptor Antagonist
KSG-504 anhydrous is a potent antagonist of the cholecystokinin (CCK) receptor. This compound has been shown to inhibit Ethionine-induced acute pancreatitis in rat models, demonstrating its relevance in studying pancreatic function and pathology. Additionally, KSG-504 facilitates the regeneration of acinar cells, making it a valuable tool for investigating therapeutic strategies in pancreatic diseases. -
CCK-B Receptor Agonist
PD-149164 is a selective agonist of the cholecystokinin B (CCK-B) receptor, exhibiting high binding affinity with IC50 values of 0.083 nM for CCK-B and 75 nM for CCK-A. This compound is instrumental in studying the role of CCK-B receptors in physiological and pathological processes, including appetite regulation, anxiety, and enhanced memory function. It serves as a valuable tool for research in neuropharmacology and gastrointestinal studies. -
CCK-4 Analog
A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (CCK-4), acting as an agonist for pancreatic amylase release. It also serves as a partial agonist, promoting phosphoinositide decomposition in pancreatic cells. With an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor, A-70874 shows a notable affinity of 1.6 μM for the CCK-B/gastrin receptor. This compound is valuable for investigating the physiological roles of CCK receptors in both the digestive system and the central nervous system. -
Cholecystokinin Receptor Antagonist
TP-680 is a potent cholecystokinin receptor antagonist, exhibiting a 1510-fold higher binding affinity for rat pancreatic CCKA receptors (IC50 = 1.2 nM) compared to rat brain CCKB receptors (IC50 = 1812.5 nM). This selectivity makes TP-680 a valuable tool for investigating gastrointestinal diseases. Its ability to modulate CCK receptor activity provides insights into gastrointestinal physiology and potential therapeutic applications in disorders related to CCK signaling. -
Cholecystokinin Antagonist
Asperlicin is a cholecystokinin antagonist derived from Aspergillus alliaceus. This compound exhibits inhibitory effects on cholecystokinin receptors, which play a crucial role in regulating gastrointestinal functions and satiety. Asperlicin is primarily utilized in research related to digestive disorders, appetite regulation, and the study of neuropeptide signaling pathways. Its ability to modulate cholecystokinin activity makes it a valuable tool for understanding gastrointestinal and metabolic processes. -
CCK-B Antagonist
L-736380 is a potent antagonist of the cholecystokinin B (CCK-B) receptor, exhibiting a high affinity with an IC50 of 0.054 nM for CCK-B and 400 nM for CCK-A. This compound effectively inhibits gastric acid secretion in anesthetized rats with an ID50 of 0.064 mg/kg. Additionally, L-736380 demonstrates significant activity in ex vivo binding assays of [125I]CCK-8S in BKTO mouse brain membranes, with an ED50 of 1.7 mg/kg. Its function as a CCK-B antagonist makes it a valuable tool for studies related to gastrointestinal physiology and neuropharmacology. -
CCK Antagonist
CCK Antagonist 1 is a potent antagonist of cholecystokinin (CCK) receptors, exhibiting IC50 values of 1.1 μM for CCK1 and 4 μM for CCK2. This compound is valuable for research into the roles of CCK in cancer and mental health disorders, facilitating the exploration of therapeutic interventions targeting these pathways. Its specificity and efficacy make it a useful tool for studying the biological functions of CCK receptors. -
CCKB/gastrin Receptor Antagonist
S-0509 is a selective antagonist of the CCKB/gastrin receptor, demonstrating potent inhibition of gastric secretion. This compound exhibits strong anti-secretory properties, making it a valuable tool in studies related to gastrointestinal health. S-0509 is particularly useful for research focused on the prevention of duodenal ulcers and the modulation of gastric acid secretion. -
CCK-8 Antagonist
LY219057 is a potent antagonist of cholecystokinin octapeptide (CCK-8), exhibiting an ID50 of 287.5 nM. This compound interferes with CCK-8 signaling pathways, making it valuable for investigating gastrointestinal and central nervous system functions. Its application spans research into appetite regulation, digestive processes, and potential therapeutic strategies for related disorders. -
CCKA Receptor Antagonist
PD-140548 is a selective cholecystokinin (CCK-A) receptor antagonist, which plays a pivotal role in modulating neuropeptide signaling. This compound has demonstrated potential in the investigation of schizophrenia and related neuropsychiatric disorders, offering insights into the CCK system's influence on behavioral outcomes. Its specificity makes it a valuable tool for elucidating the role of CCK-A receptors in various biological processes. -
CCK2 Receptor/Gastrin Antagonist
AG-041R is a selective antagonist of the CCK2 receptor and functions as a gastrin inhibitor. It effectively inhibits gastrin-induced secretion of pancreastatin with an IC50 of 2.2 nM. Additionally, AG-041R demonstrates significant anti-proliferative effects on Mastomys ECL carcinoid tumor cells, making it a valuable tool for research applications related to gastrointestinal physiology and cancer biology. -
Cholecystokinin Receptor Inhibitor
CCK-A receptor inhibitor 1 is a selective inhibitor of the cholecystokinin A (CCK-A) receptor, exhibiting a binding IC50 of 340 nM. By modulating CCK-A receptor activity, this compound plays a crucial role in studying gastrointestinal physiology and related disorders. Its inhibitory properties make it useful for research applications focused on appetite regulation and the gastrointestinal system. -
Cholecystokinin Receptor Antagonist
Gastrin/CCK Antagonist 1 is a selective antagonist of the cholecystokinin receptor (CCK). This compound plays a significant role in inhibiting the action of gastrin and CCK, making it a valuable tool for studying gastrointestinal disorders. Research applications include evaluating gastrointestinal motility, secretion, and potential therapeutic approaches for conditions associated with dysregulated CCK signaling. -
CRFR Modulator
Corticotropin-releasing factor (human) acts as a modulator of corticotropin-releasing factor receptors (CRFR). It plays a crucial role in the hypothalamic-pituitary-adrenal (HPA) axis by stimulating the synthesis and secretion of adrenocorticotropin (ACTH) in the anterior pituitary. This reagent is essential for research in stress response, neuroendocrine regulation, and related pathophysiological conditions. Its applications extend to studies in anxiety, depression, and other mood disorders, providing insight into the molecular mechanisms of HPA axis regulation. -
CRFR Agonist
Urocortin II, mouse is a selective agonist of the type-2 corticotropin-releasing factor (CRF2) receptor, exhibiting a high affinity with a Ki value of 0.66 nM for CRFR2 and over 100 nM for CRFR1. It activates CRF2 receptors via cAMP/PKA and Ca2+/CaMKII signaling pathways. This peptide is predominantly expressed in specific regions of the central nervous system and plays a crucial role in processing visceral sensory information while modulating autonomic functions, making it valuable for research in neurobiology and stress response. -
CRFR2 Antagonist
Astressin 2B is a selective antagonist of the corticotropin-releasing factor receptor 2 (CRFR2) with an IC50 of 0.57 nM. This compound disrupts the protective effects mediated by CRFR2, leading to increased intestinal damage in models of hemorrhagic injury and suggesting potential roles in studying inflammatory responses. Astressin 2B also reverses the protective effects of Urocortin 1 against intestinal complications and mitigates the anxiogenic effects of Urocortin 2, demonstrating its utility in research related to stress-induced anxiety and gastrointestinal pathology. This reagent is an effective tool for investigating CRFR2's role in intestinal protection and inflammatory processes. -
CRFR Activator
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide that primarily targets and activates CRF receptor type 2 (CRF-R2). It plays a significant role in the behavioral stress response system and is known to modulate social dynamics through its action in the medial amygdala. Urocortin III is valuable for research applications focused on stress responses and neurobehavioral studies. -
CRFR Antagonist
BMS-665053 is a potent corticotropin-releasing factor-1 (CRF1) receptor antagonist, exhibiting an IC50 of 1.0 nM. This compound effectively inhibits CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells, with an IC50 of 4.9 nM. BMS-665053 is valuable for research in neuroendocrine regulation and stress response pathways. -
CRFR2 Agonist
[DPro5] Corticotropin Releasing Factor, human, rat is a selective agonist for the CRFR2 receptor, primarily involved in neuroendocrine response regulation. This molecule stimulates the release of adrenocorticotropic hormone (ACTH) and β-endorphin, contributing to various physiological responses. Notably, unlike traditional CRF peptides, [DPro5] does not induce anxiogenic effects, instead demonstrating potential to influence learning and memory processes in rat models. It serves as a valuable tool for investigating the role of CRFR2 in stress response and cognitive function. -
CRFR Antagonist
BMS-561388 benzenesulfonate is a selective antagonist of the corticotropin-releasing factor receptor (CRFR). This compound exhibits significant potential in modulating stress-related responses, making it a valuable tool for research into neurological disorders such as anxiety and depression. Its ability to inhibit CRFR activity underscores its relevance in the study of stress-related pathologies and therapeutic interventions. -
CRFR1/2 Agonist
(Tyr0)-Urocortin, rat is a high-affinity agonist for both corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). Exhibiting inhibitory binding constants (Ki) in the range of 1-2 nM, it is a key reagent for studying the role of CRF receptors in stress response and neuroendocrine signaling. This compound is particularly valuable for research into anxiety, depression, and related disorders, facilitating investigations into receptor-mediated pathways and therapeutic interventions. -
CRFR Agonist
Sauvagine, a 40-amino-acid neuropeptide and a potent corticotropin-releasing factor (CRF) agonist, is derived from the skin of the frog. It effectively stimulates the release of adrenocorticotropic hormone (ACTH) from rat pituitary cells. Additionally, sauvagine exhibits various pharmacological effects, influencing diuresis, cardiovascular function, and endocrine activity, making it a valuable tool for research in neurobiology and endocrinology. -
CRFR Antagonist
NBI-35965 is a selective antagonist of corticotropin-releasing factor receptor 1 (CRF-R1). This compound is utilized in research applications focusing on the nervous system, particularly in studies exploring stress response, anxiety, and depression. By inhibiting CRF-R1 activity, NBI-35965 provides valuable insights into the mechanisms underlying these neuropsychiatric disorders. -
CRFR Reversible Antagonist
SN003 is a reversible antagonist of corticotropin-releasing factor receptor 1 (CRFR 1), exhibiting an IC50 of 241 nM and over 1000-fold selectivity for CRFR 1 compared to CRFR 2. This compound effectively suppresses corticotropin-releasing factor-induced adrenocorticotropic hormone (ACTH) release in vitro. Additionally, SN003 demonstrates the potential to mitigate depressive-like behavior in rat models, making it a valuable tool for research in neuropsychiatric disorders. -
CXCR Antagonist
ACT-1004-1239 is a selective antagonist of the CXCR7 receptor, exhibiting a potent inhibitory effect with an IC50 value of 3.2 nM. This compound is primarily utilized in research focused on chemokine signaling pathways and is relevant in studies investigating disorders related to the immune system and cancer. Its oral bioactivity makes it an attractive candidate for in vivo investigations targeting CXCR7-mediated pathways. -
CXCR4 Receptor Agonist
NUCC-390 dihydrochloride is a selective small-molecule agonist of the CXCR4 receptor. It promotes the internalization of CXCR4 receptors and exhibits effects that are opposite to those of conventional CXCR4 antagonists. This compound has demonstrated the potential to enhance nerve recovery following neurodegeneration in vivo, making it a valuable tool for research in neurobiology and therapeutic applications targeting nerve regeneration. -
CXCR3 Antagonist
ACT-777991 is a selective antagonist of the CXCR3 receptor, demonstrating oral bioavailability. This compound effectively inhibits the migration of activated T cells in response to CXCL11, making it a useful tool for studying immune responses and inflammatory conditions. Its stability in microsomes and hepatocytes across various animal models further supports its potential applications in pharmacological research related to autoimmune diseases and cancer immunotherapy. -
ACKR7 Agonist
VUF11207 fumarate is a selective agonist of the ACKR7 receptor (formerly known as CXCR7). This compound effectively inhibits CXCL12-induced osteoclastogenesis and bone resorption by preventing ERK phosphorylation. VUF11207 fumarate is valuable for research targeting bone metabolism and related pathologies, making it a key tool for studying the role of ACKR7 in bone homeostasis and signaling pathways. -
CXCR3 Agonist
PS372424 hydrochloride is a selective agonist of the CXCR3 receptor, a key player in immune response modulation. This compound exhibits anti-inflammatory properties by inhibiting human T-cell migration, making it valuable for research into inflammatory diseases, particularly in models of arthritic inflammation. Its ability to target CXCR3 offers insight into the therapeutic potential for treating conditions characterized by dysregulated T-cell activity. -
CXCR2/1 Antagonist
SX-517 is a dual antagonist of CXCR2 and CXCR1, featuring a boronic acid structure. It effectively inhibits CXCL1-induced calcium flux with an IC50 of 38 nM and disrupts CXCL8-induced [(35)S]GTPγS binding, showing an IC50 of 60 nM, while also preventing ERK1/2 phosphorylation. This compound demonstrates significant anti-inflammatory properties in both humanized polymorphonuclear (PMN) cells and murine models, making it a valuable tool for research into inflammation-related pathways. -
Isomer
(Rac)-Reparixin is an isomer of Reparixin and serves as a useful experimental control in research settings. Reparixin functions as a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2, exhibiting inhibitory constants (IC50) of 1 nM and 100 nM, respectively. This compound is valuable for studies focusing on inflammation, cancer biology, and other pathways mediated by chemokine signaling. -
Dual CXCR1/2 Antagonist
Ladarixin sodium is a dual antagonist of CXCR1 and CXCR2, exhibiting an allosteric non-competitive mechanism. This compound demonstrates significant anti-inflammatory activity, making it relevant for research in chronic obstructive pulmonary disease (COPD) and asthma. Its ability to inhibit CXCR1 and CXCR2 pathways positions Ladarixin sodium as a valuable tool for exploring therapeutic strategies in respiratory inflammatory conditions. -
CXCR2 Antagonist
CXCR2-IN-2 is a selective antagonist of the CXCR2 receptor, demonstrating high potency with an IC50 of 5.2 nM in a β-arrestin assay and 1 nM in the CXCR2 Tango assay. This compound exhibits significant selectivity, being approximately 730-fold more selective for CXCR2 over CXCR1 and greater than 1900-fold over other chemokine receptors. Additionally, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood with an IC50 of 0.04 μM, making it a valuable tool for research into inflammatory processes and associated therapeutic applications. -
CXCR Modulator
CXCR7 modulator 2 is a selective modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), exhibiting an affinity with a Ki value of 13 nM. This compound plays a critical role in research applications focusing on chemokine signaling pathways and their involvement in various physiological and pathological processes. It is particularly useful in studies related to cancer metastasis, inflammation, and cardiovascular diseases, making it a valuable tool for understanding CXCR7's biological functions. -
CXCR2 Antagonist
CXCR2 antagonist 8 is a potent and selective antagonist of the CXCR2 receptor, involved in inflammatory responses and immune cell migration. This compound has demonstrated significant activity in models of insulin resistance, making it a valuable tool for investigating metabolic disorders and related signaling pathways. Researchers can utilize CXCR2 antagonist 8 for studies aimed at elucidating the role of CXCR2 in various disease states. -
CXCR4 Receptor Agonist
NUCC-390 is a selective small-molecule agonist of the CXCR4 receptor. This compound induces internalization of CXCR4 receptors, thereby modulating signaling pathways distinct from antagonists. Research indicates that NUCC-390 promotes functional recovery of nerve tissue following neurodegeneration, making it a valuable tool for applications related to neurobiology and regenerative medicine. -
CXCR4 Antagonist
EPI-X4 is a selective antagonist of the C-X-C motif chemokine receptor 4 (CXCR4), exhibiting an IC50 of 8.6 μM. This compound effectively inhibits CXCL12-mediated signaling and reduces chemokine-driven migration and invasion in leukemia cells. Additionally, EPI-X4 demonstrates anti-inflammatory properties in mouse models and displays antiviral activity against CXCR4-tropic HIV, making it a valuable tool for research in cancer, inflammation, and virology. -
CXCR3 Antagonist
ACT-660602 is an orally active antagonist of the chemokine receptor CXCR3, demonstrating an IC50 value of 204 nM. This compound effectively inhibits T-cell migration, making it a valuable tool in the study of immune response. ACT-660602 has shown efficacy in models of acute lung injury and is relevant for research focused on autoimmune diseases and related inflammatory conditions. -
CXCR2 Antagonist
SB-332235 is a potent, orally active nonpeptide antagonist of the chemokine receptor CXCR2, exhibiting an IC50 of 7.7 nM and demonstrating 285-fold selectivity for CXCR2 over CXCR1. This compound has been shown to effectively inhibit both acute and chronic models of arthritis in rabbits. Additionally, SB-332235 reduces the viability of acute myeloid leukemia (AML) cells, indicating its potential utility in cancer research and therapeutic applications for inflammatory diseases. -
CXCR3 Antagonist
CXCR3 antagonist 1 is a selective and non-cytotoxic antagonist of the CXCR3 receptor, exhibiting an IC50 of 0.06 µM. This compound plays a significant role in the research of inflammatory diseases, including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes. Its ability to inhibit CXCR3 activity makes it a valuable tool for elucidating the mechanisms underlying various inflammatory conditions. -
CXCR
BVT173187 is a selective inhibitor of the CXCR target, effectively blocking the activation of the neutrophil formyl peptide receptor FPR1. This compound suppresses FPR1 agonist-induced activation in neutrophils, leading to decreased mobilization of adhesion molecules and reduced superoxide anion production. In addition to its strong effects on FPR1, BVT173187 also influences C5aR and CXCR signaling pathways, making it a valuable tool for research in inflammation and immune response. -
ELR+CXCL-CXCR1/2 Inhibitor
CXCL-CXCR1/2-IN-1 is an orally active inhibitor of the ELR+CXCL-CXCR1/2 signaling pathway, exhibiting an EC50 of 42.7 nM for the CXCR2 receptor. This compound demonstrates significant anticancer and antiangiogenic properties, making it a valuable tool for research into tumor progression and vascularization. Its ability to target these pathways underscores its potential application in cancer biology and therapeutic development. -
CXCR Antagonist
CXCR2 antagonist 2 is a potent antagonist targeting the chemokine receptor CXCR2, with an IC50 value of 95 nM. It exhibits significant biological activity by inhibiting CXCR2-mediated signaling pathways, which are implicated in cancer progression and inflammation. This reagent is particularly valuable for researchers investigating the role of CXCR2 in tumor microenvironments and the development of novel cancer immunotherapies.
