GPCR/G Protein

Items 2801-2850 of 5455

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  1. Phytocannabinoid Derivative

    Δ9-Tetrahydrocannabiorcol is a phytocannabinoid derivative that exhibits structural similarity to established cannabinoids. This compound has been studied for its interactions with the endocannabinoid system, demonstrating potential effects on cannabinoid receptors. It serves as a valuable research tool for exploring the therapeutic applications of cannabinoids in areas such as pain management, neuroprotection, and inflammation.
  2. Phytocannabinoid Derivative

    Δ9-THCH is a phytocannabinoid derivative that exhibits structural similarities to established cannabinoids. This compound interacts with the endocannabinoid system, demonstrating potential biological activity relevant to pain modulation and inflammation reduction. Research applications include studies on cannabinoid receptor signaling and the investigation of therapeutic effects in various neurobiological contexts.
  3. Cannabinoid Derivative

    CHM-FUBIATA is a synthetic cannabinoid derivative that acts primarily on the cannabinoid receptors. It exhibits notable affinity for these receptors, leading to significant alterations in neurotransmitter release and neuroprotection. This compound is utilized in research focused on understanding the pharmacological effects of cannabinoids and their potential therapeutic applications in various neurological disorders.
  4. Cannabinoid Derivative

    PB-22 N-Pentanoic acid-3-carboxyindole metabolite is a significant metabolite of the cannabinoid PB-22, primarily interacting with cannabinoid receptors. This compound exhibits notable activity in modulating cannabinoid signaling pathways and can be utilized in research applications focused on the effects of cannabinoids in neuropharmacology, pain management, and potential therapeutic interventions for various disorders related to the endocannabinoid system. Its study can enhance the understanding of cannabinoid metabolism and its biological implications.
  5. CB1 Inverse Agonist

    MRL-650 is a potent inverse agonist of the CB1 receptor, exhibiting an IC50 of 7.5 nM for CB1, while maintaining a significantly lower affinity for the CB2 receptor at 4100 nM. This compound is orally active and is primarily utilized in research focused on anorexigenic effects. Its selectivity and potency make MRL-650 a valuable tool for investigating the physiological and pharmacological roles of the endocannabinoid system.
  6. Phytocannabinoid Derivative

    iso-Hexahydrocannabinol is a phytocannabinoid derivative that interacts with the endocannabinoid system, primarily targeting cannabinoid receptors. Its unique structure allows it to exhibit biological activities similar to those of other cannabinoids, making it a valuable tool in research exploring the effects of cannabinoids on various physiological processes. Applications include studies on pain management, neuroprotection, and potential therapeutic effects in various medical conditions.
  7. Phytocannabinoid Derivative

    Δ8-iso-THC is a phytocannabinoid derivative that exhibits structural similarities to established cannabinoids. This compound engages cannabinoid receptors, demonstrating potential modulating effects on the endocannabinoid system. Δ8-iso-THC is useful for research into its therapeutic applications, including pain relief, anti-inflammatory effects, and potential neuroprotective properties. Its unique chemical structure makes it a valuable reagent for studying cannabinoid pharmacology and related therapeutic areas.
  8. Cannabinoid

    3-CAF is a synthetic cannabinoid that targets the cannabinoid receptor pathway. This compound exhibits significant activity in modulating cannabinoid receptor signaling, making it a valuable tool for investigating cannabinoid-related biological processes. Its unique 3-carboxylate-indazole structure enhances its selectivity and potency, supporting research applications in pharmacology and neurobiology focused on cannabinoid interactions and their physiological effects.
  9. Phytocannabinoid Derivative

    Cannabigerorcinic acid is a phytocannabinoid derivative that exhibits structural similarities to well-characterized cannabinoids. This compound has demonstrated potential biological activity, making it a valuable asset in the study of cannabinoid mechanisms and their physiological effects. It is particularly relevant for research focusing on the endocannabinoid system, cannabinoid receptor interactions, and potential therapeutic applications in various disorders.
  10. Cannabinoid Receptor

    Cannabiorcol, a cannabinoid receptor modulator, exhibits structural similarities to well-characterized phytocannabinoids. This compound has shown potential in influencing cannabinoid receptor activity, making it a valuable tool in cannabinoid research. Its biological activity is relevant for studies investigating the pharmacological effects of cannabinoids and therapeutic applications in various physiological conditions.
  11. BB-22 Analog

    Methyl-1-(cyclohexylmethyl)-1H-indole-3-carboxylate is an analog of BB-22, characterized by the absence of the quinoline moiety. This compound engages cannabinoid receptors, contributing to its potential as a research tool in pharmacological studies. Its unique structure supports investigations into cannabinoid signaling pathways and may aid in understanding the effects of synthetic cannabinoids. This reagent is suitable for applications in drug discovery and development within the cannabinoid research field.
  12. Cannabinoid Derivative

    5-Fluoro PB-22 5-hydroxyquinoline isomer is a synthetic cannabinoid derivative that acts primarily on cannabinoid receptors. This compound exhibits potent agonistic activity, making it valuable for research into cannabinoid receptor signaling and the pharmacological effects of synthetic cannabinoids. Its use in studies can provide insights into therapeutic applications and the modulation of endocannabinoid system functions.
  13. THJ-018 Derivative

    5-Fluoro THJ is a derivative of the synthetic cannabinoid THJ-018, targeting cannabinoid receptors in the endocannabinoid system. It exhibits biological activity that may influence neurochemical signaling and has potential applications in cannabinoid research, pharmacology, and the study of psychoactive effects. Researchers can utilize this compound to explore the mechanisms underlying cannabinoid receptor activation and its implications in various physiological processes.
  14. Semisynthetic Cannabinoid

    Δ8-THCP (Δ8-Tetrahydrocannabiphorol; n-Heptyl Δ8-THC) is a semisynthetic cannabinoid that primarily targets the CB1 receptor. It has been identified as an analytical reference standard and demonstrates significant affinity for this receptor, contributing to its potential biological activities. This compound is useful in various research applications, particularly in studies focused on cannabinoid receptor interactions and their effects.
  15. Cannabinoid Receptor Antagonist

    CB1 Antagonist 1 is a selective antagonist of the cannabinoid receptor 1 (CB1). It plays a crucial role in research pertaining to metabolic syndrome and obesity, as well as various neuroinflammatory, cognitive, and gastrointestinal disorders. Additionally, it is valuable for investigating cardiovascular conditions, making it a versatile tool in the study of endocannabinoid system-related pathways.
  16. CCK-BR Antagonist

    YM022 is a highly potent and selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor (CCK-BR). With Ki values of 68 pM for CCK-B and 63 nM for CCK-A, YM022 effectively blocks gastrin-induced gastric acid secretion and inhibits histidine decarboxylase activation in vivo. This compound is valuable for research applications related to gastrointestinal disorders and receptor signaling pathways.
  17. Dopamine D3 Receptor Antagonist

    PNU-177864 hydrochloride is a potent and selective antagonist of the dopamine D3 receptor. This compound is known to influence phospholipid metabolism in vivo and exhibits potential anti-schizophrenia activity. It serves as a valuable tool for researchers exploring the role of dopamine receptors in neurological disorders and for developing therapeutic strategies.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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