GPCR/G Protein

Items 3901-3950 of 6977

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. CCKAR Small Molecule Agonist

    CE-326597 is a small molecule agonist of the cholecystokinin A receptor (CCKAR). It selectively engages the lower region of the transmembrane domain pocket, offering unique insights into receptor activation that differ from the natural ligand CCK-8. This compound is valuable for studying metabolic disorders and gastrointestinal dysfunction, enabling researchers to explore the therapeutic potential of CCKAR modulation.
  30. CCK2R Antagonist

    CI-988 meglumin is a potent cholecystokinin 2 receptor (CCK2R) antagonist. By inhibiting CCK2R, CI-988 meglumin plays a critical role in mitigating the gastrin-mediated cardioprotective effects associated with ischemia/reperfusion injury. This compound is valuable for research in cardiac physiology and pathophysiology, particularly in studies exploring receptor signaling and myocardial stress responses.
  31. C-terminal heptapeptide of CCK

    CCK (27-33) is the C-terminal heptapeptide derived from cholecystokinin (CCK), which primarily targets CCK receptors. This peptide plays a significant role in stimulating gallbladder contraction and promoting pancreatic enzyme secretion, making it crucial for investigating digestive processes. CCK (27-33) is utilized in research applications focusing on gastrointestinal physiology and receptor signaling pathways.
  32. CCK-A Receptor Agonist

    A71378 is a selective CCK-A receptor agonist with an IC50 of 0.4 nM for the pancreatic CCK-A receptor, and significantly higher IC50 values for the cortical CCK-B and gastrin receptors at 300 nM and 1,200 nM, respectively. This compound effectively stimulates pancreatic amylase secretion with an EC50 of 0.16 nM and induces ileal muscle contraction with an EC50 of 3.7 nM. A71378 is valuable for research applications focusing on gastrointestinal pharmacology and the role of CCK-A receptors in digestive processes.
  33. CCK2 Agonist

    FE100726 is a potent Cholecystokinin 2 (CCK2) receptor agonist, exhibiting high binding affinity to the CCK2 receptor. This compound has been demonstrated to effectively stimulate gastric acid secretion in anesthetized rat models. FE100726 is valuable for research related to diabetes and gastrointestinal physiology, offering insights into the role of CCK2 signaling pathways.
  34. Cholecystokinin Receptor Inhibitor

    Gastrazole free acid is a cholecystokinin receptor antagonist that demonstrates potential in inhibiting pancreatic cancer growth. By targeting gastrin receptors, this compound plays a crucial role in the modulation of gastric functions and may aid in the investigation of therapeutic strategies for gastrointestinal malignancies. Its utility in research provides insights into receptor-mediated pathways and cancer biology.
  35. CCK2 Antagonist

    PD 136450 is a potent antagonist of cholecystokinin 2 (CCK2) receptors. This compound demonstrates significant biological activity, including anti-secretory, anxiolytic, and anti-ulcer effects. PD 136450 effectively inhibits gastric acid secretion with an IC50 of 1 mg/kg and significantly reduces hemorrhagic lesions in rat models, with an IC50 of 4.7 mg/kg. It is a valuable tool for investigating gastrointestinal disorders and evaluating potential therapeutic approaches in related pharmacological research.
  36. CCK-A/B Receptors Antagonist

    Proglumide hemicalcium is a non-peptide antagonist of cholecystokinin (CCK)-A/B receptors. It selectively inhibits the actions of CCK in the central nervous system, demonstrating key biological activities such as the inhibition of gastric secretion and protection of the gastroduodenal mucosa. Additionally, Proglumide hemicalcium exhibits antiepileptic and antioxidant properties, making it a valuable reagent for research in gastrointestinal protection and neurological studies.
  37. CCK1R Agonist

    PF-04756956 is a potent agonist of the type 1 cholecystokinin receptor (CCK1R) with an EC50 of 0.47 nM. This compound is valuable for studying the mechanisms underlying obesity and associated metabolic disorders. Its activity at CCK1R makes it a significant tool for investigating therapeutic strategies aimed at regulating appetite and metabolic function.
  38. CCK1-receptor Antagonist

    JNJ-17156516 is a potent and selective antagonist of the cholecystokinin (CCK)1 receptor. This compound demonstrates significant biological activity in inhibiting CCK-induced signaling, making it valuable for research in gastrointestinal physiology and related disorders. Its oral bioavailability positions it as a useful tool in the exploration of CCK1 receptor functions and therapeutic applications.
  39. CCKB Receptor Antagonist

    Spiroglumide is a selective cholecystokinin B (CCKB) receptor antagonist. It demonstrates significant biological activity through the inhibition of CCKB receptor signaling, making it valuable for studying the physiological roles of cholecystokinin in various biological systems. Research applications include the investigation of gastrointestinal disorders and the exploration of potential therapeutic strategies in conditions linked with dysregulated CCKB receptor activity.
  40. Cholecystokinin Receptor Agonist

    ARL 15849XX is a potent agonist of the cholecystokinin receptor, specifically designed as an analog of cholecystokinin-8 (CCK-8). It effectively engages CCK receptors, stimulating pathways associated with gastrointestinal functions and satiety. This compound is valuable in research applications focusing on digestive physiology and neuropeptide signaling pathways.
  41. Cholecystokinin Receptor Agonist

    Caerulein acetate is a decapeptide that functions as a potent agonist of the cholecystokinin receptor. It exhibits significant cholecystokinetic activity, promoting contraction of the gallbladder and facilitating bile duct function. This compound is widely used in research applications related to gastrointestinal motility and the study of digestive processes.
  42. CCKB Antagonist

    PD 135158 is a selective antagonist of the CCKB receptor, exhibiting an IC50 of 2.8 nM in mouse cortex assays. This compound demonstrates notable anxiolytic properties, making it a valuable tool for research into anxiety disorders and related neuropharmacological studies. Its specificity and potency make PD 135158 suitable for investigating the role of CCKB receptors in various biological contexts.
  43. CCK-B Antagonist

    LY262691 is a selective antagonist of the cholecystokinin B (CCK-B) receptor, known for its antipsychotic properties. This compound effectively reduces the activity of spontaneously firing A9 and A10 dopamine neurons, making it a valuable tool in antipsychotic research. Its mechanism offers insights into the modulation of dopaminergic signaling pathways related to psychiatric disorders.
  44. CCK Antagonist

    LY 202769 is a cholecystokinin (CCK) and gastrin receptor antagonist, providing a valuable tool for investigating the roles of these receptors in physiological processes. This compound exhibits potent antagonistic activity, making it suitable for research into gastrointestinal disorders as well as central nervous system diseases. Its application can aid in understanding the mechanisms of action associated with CCK and gastrin receptors in these pathologies.
  45. Cholecystokinin Receptor Antagonist

    Lorglumide is a potent cholecystokinin (CCK) receptor antagonist that effectively blocks the activity of CCK at its receptors. This compound is instrumental in studying the regulation of pancreatic secretion and growth. Lorglumide serves as a valuable tool for investigating gastrointestinal physiology and related disorders.
  46. CCK Receptor Antagonist

    Cholecystokinin (27-32)-amide is a potent antagonist of the cholecystokinin (CCK) receptor, primarily interfering with CCK-mediated signaling pathways. This compound exhibits significant biological activity in regulating digestive processes and satiety. It is widely utilized in research applications focused on gastrointestinal function, neuropeptide signaling, and potential therapeutic interventions for related disorders.
  47. CCKB/Gastrin Receptor Antagonist

    RP-69758 is a selective non-peptide antagonist of the cholecystokinin-B (CCKB)/gastrin receptor, demonstrating over 200-fold specificity for CCKB compared to CCKA receptors. This compound effectively inhibits CCK-8-induced neuronal firing in rat hippocampal slices and suppresses pentagastrin-induced gastric acid secretion in rats. RP-69758 serves as a valuable tool for investigating neurological disorders and gastrointestinal diseases in research applications.
  48. CCK Agonist

    JMV 176 is a cholecystokinin (CCK) receptor agonist that exhibits its primary activity upon initial administration. Following a period of 3–4 hours, it transitions to function as a CCK antagonist. This dual-action characteristic makes JMV 176 valuable for research exploring CCK-related physiological processes and potential therapeutic applications in gastrointestinal disorders.
  49. CCK-A Receptor Antagonist

    CHEMBL333994 is a selective antagonist of the Cholecystokinin A receptor (CCK-A receptor), exhibiting a potent inhibitory activity with an IC50 of 0.67 nM. This compound selectively targets peripheral CCK receptors and has been shown to increase CCK mRNA levels. CHEMBL333994 is useful in research related to chronic pancreatitis, providing insights into its therapeutic potential in gastrointestinal disorders.
  50. CCK-B Antagonist

    GV-150013 is a selective antagonist of the cholecystokinin B (CCK-B) receptor, known for its ability to modulate neurotransmitter activity. This compound is primarily utilized in studies investigating sleep regulation and related disorders. Its distinct mechanism of action positions GV-150013 as a valuable tool for research into the pharmacological management of sleep disturbances and anxiety-related conditions.

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