Catalog No.
Product Name
Application
Product Information
Citations
-
CXCR2/CCR7 Antagonist
CXCR2/CCR7 antagonist-1 is a potent dual antagonist of the chemokine receptors CXCR2 and CCR7, exhibiting IC50 values of 0.0046 μM and 0.0014 μM, respectively. This compound serves as a valuable tool in the investigation of cancer metastasis and the mechanisms underlying autoimmune diseases, facilitating the study of therapeutic strategies targeting these pathways. Its efficacy in inhibiting both receptors makes it suitable for a range of biochemical and pharmacological research applications. -
Dopamine D3 Receptor Antagonist
PNU-177864 is a selective, orally active antagonist of the dopamine D3 receptor. It is known to induce phospholipid metabolism in vivo and exhibits potential anti-schizophrenia effects. This compound is valuable for research focused on dopaminergic modulation and the exploration of therapeutic strategies for schizophrenia. -
CCR6/CXCR2 Antagonist
SQA1 is a squaramide derivative that functions as a CCR6 and CXCR2 antagonist, displaying a dissociation constant (Kd) of 250 nM. It effectively occupies the intracellular pocket, overlapping with the G protein binding site, which helps stabilize the closed conformation of the receptor. This compound is useful in research applications targeting chemokine receptor signaling pathways and their roles in inflammatory responses and immune cell trafficking. -
CCR5/CXCR3 Inhibitor
CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial. -
Neuropeptide
α-CGRP (mouse, rat) is a neuropeptide that primarily targets the neuromuscular junction and functions as a potent vasodilator. It is known to induce a decrease in blood pressure and an increase in heart rate upon peripheral administration, and it also promotes relaxation of colonic smooth muscle. This peptide is valuable for research applications in cardiovascular studies, pro-inflammatory responses, migraine pathophysiology, and metabolic processes. -
CGRP Receptor Antagonist
Vazegepant hydrochloride is a potent antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting a high binding affinity with a Ki value of 0.023 nM. This compound represents the first intranasal formulation in the gepant class, specifically developed for the acute management of migraine. Additionally, Vazegepant hydrochloride shows potential in addressing pulmonary inflammation associated with COVID-19, enabling further research into its therapeutic applications in these areas. -
Calcitonin Peptide
β-CGRP, human is a member of the calcitonin peptide family and functions through binding to the calcitonin-receptor-like receptor (CRLR) in conjunction with receptor-activity-modifying proteins (RAMPs). It exhibits high affinity, with IC50 values of 1 nM for the CRLR/RAMP1 complex and 300 nM for the CRLR/RAMP2 complex in cellular assays. This peptide is crucial for research in pain modulation, migraine mechanisms, and neurobiological studies. -
CGRP Antagonist
Atogepant is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting potent oral bioavailability. It is primarily utilized in research related to migraine pathophysiology and therapeutic interventions, contributing to the understanding of CGRP’s role in migraine mechanisms. This compound enables detailed investigations into migraine relief strategies targeting CGRP signaling pathways. -
CGRP Receptor Antagonist
Vazegepant is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist. It selectively inhibits the CGRP receptor, thereby modulating pain pathways associated with migraine. This compound is valuable for research on migraine treatments and the role of CGRP in nociceptive signaling. -
CGRP Receptor Activator
Adrenomedullin (1-50), rat is a 50 amino acid peptide that functions as a CGRP receptor activator. It is known to induce selective arterial vasodilation, making it relevant for research in cardiovascular physiology and pathophysiology. This peptide is utilized in studies investigating the role of adrenomedullin in vascular regulation and its potential therapeutic applications in hypertension and related disorders. -
CGRP Receptor Antagonist
Rimegepant sulfate hydrate is a potent, orally active, selective antagonist of the calcitonin gene-related peptide (CGRP) receptor. It exhibits a binding affinity with a Ki of 0.027 nM and an IC50 of 0.14 nM for the human CGRP receptor. This compound is primarily utilized in migraine research, contributing to studies focused on novel therapeutic approaches for migraine management. -
hADM Analog
Adrenomedullin (16-31), human is a peptide fragment comprising amino acid residues 16-31 of human adrenomedullin (hADM). This analog exhibits significant affinity for the CGRP1 receptor, influencing cardiovascular regulation. It has been shown to elicit pressor activity in the systemic vascular bed of rats, making it a valuable tool for exploring vascular responses and related research applications. -
CGRP Receptor Antagonist
HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist that plays a significant role in the study of migraine pathology. It effectively inhibits CGRP receptor activity, which is critical for understanding migraine mechanisms and developing therapeutic strategies. HTL22562 is primarily used in acute research settings to explore the implications of CGRP signaling in headache disorders. -
CGRP Antagonist
CGRP Antagonist 7 is a highly potent calcitonin gene-related peptide (CGRP) receptor antagonist, exhibiting a Ki value of 0.029 nM. This compound effectively inhibits the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP Antagonist 7 is primarily utilized in research focused on migraine pathophysiology and therapeutic interventions targeting CGRP signaling pathways. -
CGRP Receptor Antagonist
MK-8825 is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating a Ki value of 47 pM for human and 17 nM for rat receptors. It effectively inhibits CGRP-mediated cAMP responses, showcasing competitive antagonism. This compound is valuable for research into migraine and temporomandibular joint disorders, contributing to the understanding of therapeutic targets in these conditions. -
CGRP Receptor Antagonist
Rimegepant hemisulfate is a selective and competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting a Ki value of 0.027 nM and an IC50 of 0.14 nM for the human CGRP receptor. This compound demonstrates potent biological activity in blocking CGRP signaling pathways, making it a valuable tool for migraine research and the investigation of related neurological conditions. Its oral bioavailability supports its application in in vivo studies focused on migraines and CGRP-mediated mechanisms. -
CGRP Receptor Antagonist
Desfluoro-BMS-694153 is a potent antagonist of the calcitonin gene-related peptide (CGRP) receptor, with a Ki value of 0.01 nM. This compound exhibits minimal risk of CYP3A4 inhibition, demonstrated by IC50 values of 36 μM for CYP3A4-BFC and 6 μM for CYP3A4-BZR. Desfluoro-BMS-694153 is primarily utilized in research focused on migraine pathophysiology and the exploration of therapeutic interventions targeting CGRP pathways. -
Fragment of Pro-Adrenomedullin
Adrenotensin (human), a fragment of pro-adrenomedullin, corresponds to amino acids 153-185 of the precursor peptide. As a member of the calcitonin gene-related peptide (CGRP) superfamily, Adrenomedullin (ADM) functions as a multifunctional vasoactive hormone. This fragment is relevant for research applications targeting cardiovascular physiology, cellular signaling, and pathophysiological processes associated with ADM. -
CGRP Antagonist
BMS-846372 is a potent oral antagonist of the calcitonin gene-related peptide (CGRP), exhibiting a Ki value of 0.07 nM. This compound is primarily utilized in research studies focused on migraine pathophysiology and may aid in the development of therapeutic strategies for migraine management. -
CGRP Antagonist
CGRP Antagonist 2 is a competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor. It effectively inhibits CGRP-mediated signaling, which is crucial for the modulation of nociceptive pathways associated with pain perception. This reagent is widely utilized in research focused on migraine mechanisms and pain management therapies. -
CGRP Receptor Activator
Calcitonin Gene Related Peptide II (rat) is a CGRP receptor activator that functions as a potent and enduring vasodilator. It plays a crucial role in the regulation of vascular tone and blood pressure. This peptide is utilized in research on cardiovascular diseases, aiding in the exploration of therapeutic strategies for conditions such as hypertension and vascular dysfunction. -
CGRP Receptor Agonist
Calcitonin (salmon) (acetate) functions as a calcitonin gene-related peptide (CGRP) receptor agonist. This compound stimulates bone formation while inhibiting bone resorption, making it valuable for research in osteoporosis and other bone-related disorders. The acetate form enhances the absorption and bioactivity of the peptide, providing a more effective hormonal intervention for studies focusing on bone metabolism and calcium homeostasis. -
Active Compound
Adrenomedullin (11-50), rat is a bioactive peptide fragment that represents the C-terminal portion of rat adrenomedullin. This compound primarily targets CGRP1 receptors, effectively inducing selective arterial vasodilation. Its key biological activity makes it useful in cardiovascular research, particularly in studies focusing on vascular function and regulation. -
CGRP Receptor Antagonist
BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP receptor). This compound exhibits significant biological activity in blocking CGRP-mediated signaling pathways, making it a valuable tool for migraine research. It is particularly effective in studies examining intranasal delivery methods for rapid therapeutic intervention in migraine treatment. -
Stable Isotope
Telcagepant-d8 is a deuterium-labeled variant of Telcagepant, a potent orally active antagonist of the calcitonin gene-related peptide (CGRP) receptor. This compound exhibits binding affinities (Kis) of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively. Telcagepant-d8 is primarily utilized in pharmacokinetic studies and metabolic research, providing a valuable tool for investigating CGRP-related pathways and receptor interactions in various biological systems. -
CCKBR Agonist
CCKBR agonist-1 is a potent agonist of the cholecystokinin B receptor (CCKBR), preferentially activating Gq-proteins with an EC50 of 35 pM. This compound enhances neuronal survival, demonstrated by an EC50 of 37 pM, and has shown efficacy in mitigating cognitive decline in murine models. Mechanistically, CCKBR agonist-1 upregulates α-secretase (ADAM10) and the calcium signaling molecule PLCB4, leading to decreased amyloid β (Aβ) plaque formation and enhancement of long-term potentiation (LTP). CCKBR agonist-1 serves as a valuable tool for research into Alzheimer's disease. -
CCKBR Agonist
CCKBR agonist-2 is a selective agonist for the cholecystokinin B receptor (CCKBR), primarily activating the Gi signaling pathway with an EC50 of 0.27 nM. This compound demonstrates minimal interaction with Gq and Gs pathways, making it a valuable tool for studying Gi-mediated cellular responses. Despite its potency in activating CCKBR-Gi signaling, CCKBR agonist-2 does not exhibit significant neuroprotective effects in mouse models of Alzheimer's disease, highlighting the complexity of cognitive function modulation. This reagent is useful in research exploring the roles of CCKBR signaling in various physiological and pathological contexts. -
CCK Receptor Antagonist
Devazepide is a potent, competitive, and selective antagonist of the cholecystokinin (CCK) receptor. It exhibits high affinity with IC50 values of 81 pM, 45 pM, and 245 nM for rat pancreatic, bovine gallbladder, and guinea pig brain CCK receptors, respectively. This nonpeptide agent is primarily utilized in research focused on gastrointestinal disorders, providing insights into gastrointestinal physiology and the therapeutic potential of CCK receptor modulation. -
CCK-B Antagonist
L-365260 is a selective antagonist of the cholecystokinin B receptor (CCK-B), exhibiting high affinity with Ki values of 1.9 nM for non-peptide gastrin and 2.0 nM for brain CCK receptors. It engages competitively and stereoselectively with these receptors, making it valuable in studies of neuropharmacology. Additionally, L-365260 has been shown to enhance morphine analgesia while preventing the development of morphine tolerance, highlighting its potential utility in pain management research. -
Cholecystokinin Receptor Antagonist
Lorglumide sodium is a potent cholecystokinin (CCK) receptor antagonist that inhibits the action of CCK, a peptide hormone involved in digestion and satiety. Its antagonistic properties make it useful in research applications related to gastrointestinal function, appetite regulation, and the modulation of pain pathways. Lorglumide sodium serves as a valuable tool for studying CCK receptor-mediated signaling and related biological processes. -
CCKA Agonist
A71623 is a potent and highly selective full agonist for the CCK-A receptor, demonstrating a strong affinity with an IC50 of 3.7 nM in guinea pig pancreatic tissues and minimal activity at CCK-B receptors with an IC50 of 4500 nM. Its selectivity makes A71623 a valuable tool for studying CCK-A receptor functions and related physiological processes. This compound is applicable in research exploring gastrointestinal physiology, neurobiology, and the modulation of satiety signaling pathways. -
CCK1 Receptor Antagonist
Lintitript is a highly potent and selective non-peptide antagonist of the cholecystokinin (CCK1) receptor, exhibiting an EC50 of 6 nM and a Ki value of 0.2 nM. It demonstrates over 33-fold selectivity for CCK1 compared to CCK2 receptors, which have an EC50 of 200 nM. This compound is significant in research applications focused on appetite regulation, as it increases plasma concentration of leptin and insulin, thereby influencing food intake. -
CCK2 Antagonist
PNB-001 is a selective antagonist of the cholecystokinin receptor type 2 (CCK2), demonstrating significant anti-inflammatory and analgesic properties. This compound is particularly valuable in research focused on pain management and inflammation pathways. Its oral bioactivity makes it a suitable candidate for in vivo studies examining CCK2 modulation in various biological systems. -
Cholecystokinin Receptor Antagonist
T-0632 is a potent cholecystokinin (CCK) A receptor antagonist that effectively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors, demonstrating a K_i value of 0.24 nM. It shows significant selectivity in blocking CCK-8-induced pancreatic enzyme release, with an IC_50 value of 5.0 nM. T-0632 exhibits reversible antagonistic effects in rabbit gallbladder smooth muscle, distinguishing it from other CCK A antagonists. This compound is valuable for researching the physiological roles of CCK receptors and their impact on gastrointestinal function. -
Cholecystokinin Receptor Antagonist
LY 225910 is a selective antagonist of the cholecystokinin receptor (CCK2 receptor), primarily impacting the excitatory response associated with morphine. By inhibiting this receptor, LY 225910 plays a significant role in morphine sensitization, making it a valuable tool in research focused on pain management and addiction. Its application can aid in understanding the mechanisms underlying opioid response and potential therapeutic strategies. -
Cholecystokinin Receptor Antagonist
Pranazepide is a selective antagonist of the cholecystokinin-A receptor (CCK-A), implicated in regulating gastrointestinal functions and satiety. This compound exhibits significant biological activity by modulating neural signaling pathways associated with appetite control and gastrointestinal motility. Pranazepide is commonly utilized in pharmacological research focused on obesity, anxiolytic effects, and the role of CCK in the central nervous system. -
CCK2 Receptor Antagonist
JNJ-26070109 is a selective antagonist of the cholecystokinin 2 (CCK2) receptor, exhibiting high-affinity and competitive binding. With favorable pharmacokinetic properties, it demonstrates pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. This compound is particularly relevant for research into gastroesophageal reflux disease, as CCK2 receptors play a dual role in regulating gastric acid secretion and the growth of gastrointestinal mucosa. -
CCK Derivative
Cholecystokinin Octapeptide, desulfated TFA is a synthetic derivative of the endogenous hormone cholecystokinin (CCK), which primarily targets CCK receptors. This peptide exhibits key biological activities related to digestion and satiety regulation, making it valuable in studies of gastrointestinal physiology and appetite control. It is frequently utilized in research applications investigating the role of CCK in various biological processes, including pancreatic enzyme secretion and gastric motility. -
Cholecystokinin Receptor Antagonist
A-65186 is a cholecystokinin (CCK) A receptor antagonist that effectively inhibits CCK8-induced amylase secretion. This compound exhibits high binding affinity for pancreatic CCK-A receptors and demonstrates over 500-fold selectivity for CCK-A over CCK-B receptors. It serves as a valuable tool in research focused on gastrointestinal physiology and the role of CCK signaling in pancreatic function. -
Cholecystokinin Receptor Antagonist
(Rac)-Sograzepide functions as an antagonist of the cholecystokinin B (CCK-B) receptor, effectively inhibiting its activity. This compound is primarily utilized in research focused on modulating gastric acid secretion and exploring potential therapeutic strategies for gastrointestinal disorders. Its role in receptor inhibition makes it valuable for studies related to the regulation of digestive processes and related physiological pathways. -
Peptide Hormone
CCK (26-31) sulfated is a peptide hormone fragment that plays a crucial role in gastrointestinal function and neuroendocrine signaling. This bioactive peptide is involved in stimulating digestive processes, modulating appetite, and influencing anxiety-related behavior. Research applications include studies on gut-brain interactions, appetite regulation, and the pharmacological effects of peptide hormones in both physiological and pathological contexts. -
Gastrin/CCK-B Antagonist
CCK-B Receptor Antagonist 2 is a potent antagonist of the Gastrin/CCK-B receptor, exhibiting an IC50 of 0.43 nM. This compound also demonstrates inhibitory activity against the gastrin/CCK-A receptor with an IC50 of 1.82 μM. CCK-B Receptor Antagonist 2 serves as a valuable tool for research on gastrointestinal signaling and modulation of gastrin-related pathways, making it significant for studies concerning gastric function and disorders. -
Cholecystokinin Receptor Antagonist
Tarazepide is a potent antagonist of the cholecystokinin A (CCK-A) receptor. This compound inhibits CCK-A mediated signaling, demonstrating significant biological activity in modulating gastrointestinal functions and appetite regulation. Tarazepide is utilized in research applications related to digestion, metabolic disorders, and neurobiology, making it a valuable tool for studying the role of CCK receptors in various physiological processes. -
CCKB Receptor Antagonists
Pentagastrin meglumine is a selective antagonist of the Cholecystokinin B (CCKB) receptor, exhibiting an IC50 of 11 nM for CCKB and 1100 nM for CCKA. It plays a significant role in enhancing gastric mucosal defense mechanisms against acidity and provides protective effects on the gastric mucosa from experimental injury. This compound is valuable for research applications focused on gastrointestinal health and pathology. -
CCK2/gastrin Receptor Antagonist
Gastrazole is a potent and selective antagonist of the CCK2/gastrin receptor. This compound effectively reduces gastric acid levels and has been shown to inhibit gastrin-stimulated growth in pancreatic cancer cells. As such, Gastrazole is a valuable tool for research focused on gastrointestinal disorders and cancer biology. -
CCK2R Antagonist
GV150013X is a potent antagonist of the cholecystokinin-2/gastrin receptor (CCK2R), exhibiting a Ki value of 2.29 nM. This compound has demonstrated efficacy in attenuating central nervous system disorders, particularly in models of anxiety and panic disorder. Its application in research may provide valuable insights into the therapeutic potential for CCK2R modulation in neuropsychiatric conditions. -
CCK-B Receptor Antagonist
RP 72540 is a selective antagonist of the CCK-B receptor, exhibiting IC50 values of 2.4 nM, 1.2 nM, and 3.8 nM in guinea pig, rat, and mouse cerebral cortices, respectively. This compound effectively inhibits CCK-8-induced neuronal firing and demonstrates a dose-dependent reduction in gastric acid secretion. RP 72540 serves as a valuable tool in research applications aiming to elucidate the physiological roles of CCK-B receptors, particularly in the context of gastrointestinal processes and neurophysiology. -
Cholecystokinin Receptor
CI-1015 is a potent antagonist of the cholecystokinin B (CCK-B) receptor, which plays a critical role in gastrointestinal physiology and neurotransmission. This compound effectively inhibits CCK-B receptor activity, making it valuable for research into gastrointestinal disorders, anxiety, and pain modulation. Its specificity for the CCK-B receptor allows for the exploration of therapeutic avenues in conditions where CCK signaling is implicated. -
Appetite Suppressant
Ro 23-7014 is a cholecystokinin (CCK-7) analog that functions as an appetite suppressant. This compound modulates the central and peripheral pathways involved in energy homeostasis, making it valuable for research on obesity and metabolic disorders. Its ability to influence feeding behavior positions Ro 23-7014 as a relevant tool for exploring therapeutic targets in appetite regulation and weight management studies. -
Cholecystokinin Receptor
Mini Gastrin I, human is a truncated form of human gastrin, comprising amino acids 5-17 of the full peptide. It primarily targets the cholecystokinin receptor, playing a crucial role in gastrointestinal function by stimulating gastric acid secretion and promoting digestive enzyme release. This reagent is valuable for research in gastrointestinal physiology and the study of receptor signaling pathways associated with gastrin.
