GPCR/G Protein

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  1. Somatostatin Receptor Agonist

    L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. This compound facilitates the exploration of somatostatin receptor physiological functions, contributing to a better understanding of its role in various biological processes. It is useful for research applications aimed at studying neuroendocrine regulation and potential therapeutic targets related to somatostatin signaling.
  2. Somatostatin Neuropeptide

    Cortistatin-29 (human) is a somatostatin neuropeptide that modulates a variety of biological functions by interacting with somatostatin receptors. This compound exhibits key biological activities, including anti-inflammatory effects and regulation of pain pathways, making it relevant for research applications in cancer, inflammation, autoimmunity, fibrosis, and pain management. Its unique biological profile allows for exploration of potential therapeutic strategies targeting these conditions.
  3. Somatostatin Receptors Activator

    Veldoreotide is a somatostatin receptor activator that selectively binds to and activates somatostatin receptors 2, 4, and 5. This compound effectively inhibits growth hormone secretion in adenomas, presenting a potential advantage over other somatostatin analogues. Additionally, Veldoreotide may serve as a pain modulating agent, making it relevant for research in endocrine disorders and pain management strategies.
  4. Somatostatin Agonist

    Pasireotide pamoate is a long-acting somatostatin analogue that primarily targets somatostatin receptors (sst1/2/3/4/5) with notable binding affinity (pKi=8.2/9.0/9.1/<7.0/9.9). This compound demonstrates significant antisecretory, antiproliferative, and proapoptotic properties, making it valuable for research on neuroendocrine tumors and disorders related to dysregulated hormone secretion. Its diverse biological activities support investigations into therapeutic approaches for various endocrine-related pathologies.
  5. Somatostatin (1-28) Derivative

    [Nle8] Somatostatin (1-28) is a derivative of somatostatin (1-28) in which norleucine substitutes for methionine at position 8. This compound enhances amylase release and elevates cyclic AMP levels in pancreatic acini. It is utilized in research to study pancreatic function and the regulatory mechanisms of peptide hormones in metabolic processes.
  6. Somatostatin Enhancer

    FK962 is a somatostatin enhancer that stimulates the release of this neuropeptide, leading to cognitive-enhancing effects. Its potential anti-dementia properties make it a valuable compound for research focused on neurological diseases and cognitive disorders. Studies exploring FK962 may contribute to a better understanding of somatostatin's role in neuroprotection and cognitive function.
  7. Somatostatin Receptor Antagonist

    PRL 3195 is a somatostatin receptor antagonist that exhibits inhibition constants (Kis) of 6, 17, 66, 1000, and 1000 nM for human somatostatin receptors sst5, sst2, sst3, sst1, and sst4, respectively. This compound is utilized in research to investigate the role of somatostatin signaling in various physiological and pathological processes. Its selective blockade of somatostatin receptors makes it a valuable tool for studying neuroendocrine regulation and potential therapeutic applications in disorders involving somatostatin dysregulation.
  8. Somatostatin Receptor 5 Agonist

    BIM 23052 is a selective agonist for the somatostatin receptor 5 (SSTR5). It has been shown to enhance gastric emptying, making it a valuable tool for research in gastrointestinal function and disorders. This compound is of particular interest in studies investigating the regulatory mechanisms of hormone action and potential therapeutic applications in gastric motility disorders.
  9. Somatostatin Receptor

    [Tyr1]-Somatostatin-14 is a bioactive peptide that specifically targets the somatostatin receptor subtype 2 (SSTR2). This compound exhibits high binding affinity, making it a crucial tool for studying receptor signaling pathways and somatostatin-mediated biological processes. Its applications extend to cancer research, neurobiology, and endocrine function studies, allowing researchers to explore therapeutic interventions and physiological mechanisms involving somatostatin receptors.
  10. Somatostatin Analog

    (D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide is a somatostatin analog that demonstrates selective binding affinity with Kd values of 0.61 nM for SSTR5, 11.05 nM for SSTR3, 23.5 nM for SSTR2, 1200 nM for SSTR1, and >1000 nM for SSTR4. This compound exhibits significant biological activity relevant to the regulation of hormonal secretion and inhibition of tumor growth. It is suitable for research applications investigating the role of somatostatin receptors in various physiological and pathological processes.
  11. Human Somatostatin Receptor Antagonist

    BN-81674 is a selective antagonist targeting the human somatostatin sst3 receptor, exhibiting a Ki of 0.92 nM. This compound effectively reverses the inhibition of cyclic AMP accumulation caused by somatostatin at nanomolar concentrations, with an IC50 value of 0.84 nM. BN-81674 is suitable for applications in cancer research, particularly in studies assessing somatostatin signaling pathways and their implications in tumor biology.
  12. Somatostatin-28 Analog

    [Leu8,D-Trp22,Tyr25] Somatostatin-28 is an analog of somatostatin-28, a peptide that plays a critical role in inhibiting hormone secretion and regulating various physiological functions. This modified form enhances the stability and potency of its biological activity, making it useful in research related to neuroendocrine signaling and metabolic regulation. Applications include studying cell signaling pathways, hormonal regulation, and potential therapeutic effects on neuroendocrine tumors.
  13. Somatostatin Analog

    RC-160 [Lys(Boc)] is an 8-amino acid peptide analog of somatostatin, which primarily acts on somatostatin receptors. It exhibits significant activity in inhibiting hormone secretion and has potential applications in research focused on neuroendocrine regulation and tumor biology. This compound serves as a valuable tool for studying the physiological effects of somatostatin and its analogs in various biological systems.
  14. Somatostatin Receptor Antagonist

    BIM-23056 TFA is a linear octapeptide that serves as a potent antagonist of the somatostatin receptors sst3 and sst5, exhibiting Ki values of 10.8 nM and 5.7 nM, respectively. It effectively inhibits somatostatin-mediated signaling, making it a valuable tool for studying the physiological roles of somatostatin receptors in various biological processes. This compound is suitable for research applications involving endocrine function and neuroendocrine tumor studies.
  15. Somatostatin Agonist

    Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a potent somatostatin agonist that selectively activates somatostatin receptors. It demonstrates significant biological activity in modulating hormone secretion and inhibiting cellular proliferation. This compound is primarily utilized in cancer research, particularly in studies focused on tumor growth regulation and neuroendocrine function.
  16. Somatostatin Analogue

    Axareotide is a synthetic analogue of somatostatin that acts primarily on somatostatin receptors. It is known for its inhibitory effects on hormone secretion, particularly growth hormone and insulin. Axareotide is utilized in research focused on neuroendocrine tumors, acromegaly, and other conditions associated with abnormal hormone levels, providing valuable insights into somatostatin signaling pathways.
  17. Somatostatin Analogue

    Wy 41747 is a long-acting somatostatin analogue that primarily targets somatostatin receptors. This compound exhibits significant biological activity in modulating hormone secretion and is primarily utilized in research focused on diabetes mellitus and related endocrine disorders. Its prolonged action enables detailed studies of the physiological effects and therapeutic potential of somatostatin analogues in metabolic diseases.
  18. Somatostatin Receptor Agonist

    L-779976 is a somatostatin receptor agonist that exhibits notable anxiolytic effects. When administered into the amygdala and septum of rat brains, it has been shown to modulate anxiety-related behaviors through its complex interactions with somatostatin receptors. This compound is instrumental in research applications focusing on anxiety disorders and neuropharmacology, enabling the investigation of somatostatin's role in stress responses and emotional regulation.
  19. Somatostatin Receptor Inhibitor

    SRA880 free base is a somatostatin receptor inhibitor, specifically targeting the somatostatin-1 autoreceptor. This compound exhibits antidepressant-modulating effects and has been shown to enhance the efficacy of imipramine, resulting in antidepressant-like outcomes. Additionally, SRA880 influences brain-derived neurotrophic factor (BDNF) mRNA expression and modulates the phosphorylation of associated proteins, making it a valuable tool in neurobiological research focusing on mood disorders and related pathways.
  20. Somatostatin Analog

    Ilatreotide is a potent somatostatin analog known for its improved oral bioactivity. It effectively suppresses both fasting and postprandial secretion of various gastrointestinal and pancreatic hormones. This compound is valuable for research into gastroenteropancreatic tumors and offers insights into hormonal regulation in related pathologies.
  21. Somatostatin Receptor Agonist

    SSTR4 Agonist 5 is a potent, orally active agonist of the somatostatin receptor 4 (SSTR4) with an EC50 value of 0.228 nM. Demonstrating considerable stability in human and rat liver microsomes, this compound has shown effectiveness in inhibiting mechanical hyperalgesia in rat models. It is a valuable tool for research applications involving pain mechanisms and SSTR4-related pathways.
  22. Somatostatin Receptor Agonist

    L-054522 is an agonist for somatostatin receptor subtype 2, featuring a Kd of 0.01 nM. This compound effectively inhibits growth hormone secretion from rat primary pituitary cells with an IC50 of 0.05 nM, as well as glucagon and insulin release from isolated mouse pancreatic islet cells, exhibiting IC50 values of 0.05 nM and 12 nM, respectively. L-054522 serves as a valuable tool for exploring somatostatin signaling and its impact on endocrine functions in research applications.
  23. Somatostatin Analogue

    (D-Trp8,D-Cys14)-Somatostatin-14 is a synthetic analogue of somatostatin, targeting somatostatin receptors. This peptide exhibits significant biological activity in modulating hormonal secretion and inhibiting cell proliferation, making it valuable in research related to metabolic disorders and neuroendocrine tumors. Its unique structure allows for enhanced stability and potency in various biological assays.
  24. Somatostatin Receptor Inhibitor

    Des-threoninol-octreotide is a potent somatostatin receptor inhibitor, primarily targeting the mSSTR2b, rSSTR5, and hSSTR5 receptor subtypes. This compound demonstrates high inhibitory activity with IC50 values of 13.62 nM, 10.63 nM, and 10.95 nM, respectively. It is valuable for research applications exploring neuroendocrine regulation, peptide hormone signaling, and potential therapeutic interventions involving somatostatin pathways.
  25. Somatostatin Agonist

    Pasireotide (diaspartate) is a long-acting somatostatin agonist targeting somatostatin receptors sst1, sst2, sst3, sst4, and sst5, with pKi values of 8.2, 9.0, 9.1, <7.0, and 9.9, respectively. This cyclohexapeptide compound demonstrates significant antisecretory, antiproliferative, and proapoptotic activities. Its diverse biological effects make it a valuable tool for research applications in endocrinology and oncology, particularly in the study of neuroendocrine tumors and hormonal regulation.
  26. Somatostatin Analogue

    Nendratareotide is a somatostatin analogue that primarily targets somatostatin receptors. It exhibits inhibitory effects on hormone secretion, making it valuable in the treatment of neuroendocrine tumors and acromegaly. This compound is also utilized in research focused on understanding the physiological roles of somatostatin and its impact on glucose metabolism and cell proliferation.
  27. Somatostatin Analogue

    [D-Trp8,Tyr11] Somatostatin is a somatostatin analogue that enhances the hormone's stability and bioactivity. This compound is known to inhibit the secretion of growth hormone and other hormones, making it valuable in studies related to hormonal regulation and physiological processes. Applications include endocrynology research and the investigation of tumor growth inhibition, particularly in neuroendocrine tumors.
  28. Somatostatin-28 (1-14) Analogue

    [Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) that targets somatostatin receptors to modulate neuropeptide signaling. This peptide fragment plays a crucial role in the regulation of various physiological processes, including hormone secretion and cell proliferation. It is commonly used in research applications focused on neuroendocrine signaling pathways and therapeutic interventions for endocrine-related disorders.
  29. Somatostatin Analog

    AP102 is a dual somatostatin receptor analogue targeting SSTR2 and SSTR5. This disulfide-bridged octapeptide exhibits subnanomolar affinity for SSTR2 and SSTR5, with IC50 values of 0.63 nM and 0.65 nM, respectively, while showing no binding to SSTR1 or SSTR3. AP102 is particularly valuable in research related to acromegaly and neuroendocrine tumors, providing insights into receptor-specific signaling pathways.
  30. Somatostatin Receptor Agonist

    Zavolosotine is an orally active agonist of the somatostatin receptor type 5 (SST5), exhibiting a potent EC50 of less than 1 nM. This compound effectively inhibits insulin and glucagon secretion while also elevating glucagon levels in a rat model. Zavolosotine is valuable for research in glucose metabolism and endocrine signaling pathways, making it a key reagent for studies on metabolic disorders and diabetes.
  31. Urotensin II Anague

    Urotensin II-related peptide is an analog of human urotensin II, exhibiting high affinity for the urotensin II receptor (UT). This peptide plays a significant role in cardiovascular regulation and may influence vascular smooth muscle contraction. It is commonly utilized in research focused on cardiovascular diseases, neurobiology, and the study of peptide receptor interactions.
  32. Urotensin Receptor Antagonist

    SB-611812 is a selective antagonist of the urotensin II receptor (UTR), which plays a significant role in cardiovascular regulation. This compound is useful in investigating the pathological mechanisms underlying cardiovascular diseases and may aid in the development of novel therapeutic strategies targeting UTR-mediated pathways. Researchers can utilize SB-611812 to explore its effects on vascular function and cardiac remodeling in experimental models.
  33. Urotensin II Receptor Antagonist

    SB-706375 is an antagonist of the Urotensin II (UII) receptor, which plays a key role in renal physiology. By inhibiting this receptor, SB-706375 effectively decreases the kidney's response to UII and Urotensin-related peptide (URP), leading to a significant increase in Glomerular Filtration Rate (GFR). This compound is valuable for research applications focused on kidney diseases and hypertension, facilitating further understanding of renal function and associated pathologies.
  34. Urotensin-II Receptor Antagonist

    GSK 1562590 hydrochloride is a potent and selective antagonist of the urotensin-II receptor (UT), exhibiting pKi values ranging from 9.14 to 9.66 across various mammalian species, including mouse, rat, cat, monkey, and human. This compound demonstrates significant inhibition of UT-mediated signaling pathways, making it valuable for research into cardiovascular and neuroendocrine disorders associated with urotensin-II. Its high affinity and selectivity position GSK 1562590 as an essential tool for studying the role of urotensin-II in physiological and pathological processes.
  35. urotensin-II Receptor Antagonist Peptide

    Urantide is a selective and competitive antagonist of the urotensin-II (UT) receptor, exhibiting a pKB of 8.3. This peptide effectively inhibits human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide is valuable for investigating the (patho)physiological roles of hU-II in the mammalian cardiovascular system, making it an important tool for related research applications.
  36. Urotensin Receptor Agonist

    Urotensin II (114-124), human, is a peptide comprising 11 amino acids that functions as a potent vasoconstrictor and an agonist for the urotensin receptor (GPR14). This compound is utilized in research to explore cardiovascular function and pathophysiology, particularly regarding its role in regulating vascular tone and blood pressure. Its biological activity makes it a valuable tool for studying urotensin signaling pathways and their implications in various disease states.
  37. Urotensin II Antagonist

    Palosuran hydrochloride is a selective, orally active antagonist of the urotensin II receptor, exhibiting an IC50 of 3.6 nM in CHO cell membranes expressing human recombinant receptors. This compound demonstrates potential to improve pancreatic and renal function in diabetic models, making it a valuable tool for research in metabolic and renal disorders. Its mechanism and target highlight its relevance in studies of urotensin II signaling pathways.
  38. Urotensin Receptor Agonist

    AC-7954 free base is a selective nonpeptidic agonist of the urotensin receptor, demonstrating an EC50 of 300 nM at the human urotensin II receptor. This compound is valuable for research focused on the urotensin signaling pathway and its implications in cardiovascular and metabolic disorders. Its specificity makes it suitable for studies investigating the physiological and pathological roles of urotensin receptors in various biological systems.
  39. Urotensin Receptor Agonist

    AC-7954 is a selective nonpeptidic agonist of the urotensin receptor, exhibiting an EC50 of 300 nM at the human urotensin II receptor. This compound plays a significant role in cardiovascular and metabolic research, with potential applications in the study of hypertension and heart failure. AC-7954 can be utilized to explore urotensin-related signaling pathways and their implications in various physiological processes.
  40. Urotensin Receptor Antagonist

    SB-436811 is a selective antagonist of the urotensin-II receptor, exhibiting a pKi value of 6.7. This compound is primarily utilized in research focused on cardiovascular and metabolic disorders, where the urotensin-II pathway plays a significant role. By inhibiting urotensin-II activity, SB-436811 can aid in the exploration of its physiological effects and potential therapeutic applications.
  41. Endothelin A Receptor Antagonist

    JKC 301 is a selective Endothelin A receptor antagonist that effectively mitigates the pressor effects of nicotine in rat models. This compound is particularly valuable for investigating the cardiovascular diseases associated with smoking. Its targeted mechanism makes JKC 301 a useful tool for researchers studying the pathophysiological effects of nicotine on cardiovascular function.
  42. Precursor of Endothelin-1

    Big Endothelin-1 (1-39), porcine is the precursor peptide of endothelin-1 (ET-1), a potent vasoconstrictor significantly involved in cardiovascular regulation. This reagent exhibits similar pressor effects in vivo, making it valuable for studies investigating vascular function and regulation. It is useful in research applications that aim to elucidate the roles of endothelin peptides in physiological and pathological processes.
  43. platelet aggregation inhibitor

    Trifenagrel is an orally active platelet aggregation inhibitor that targets the pathways induced by arachidonic acid and collagen. It demonstrates significant biological activity, with ED50 values of 1.4 mg/kg and 9.4 mg/kg for the inhibition of AA- and collagen-induced platelet aggregation in guinea pigs, respectively. This compound serves as a valuable tool in cardiovascular research and the study of thrombotic disorders.
  44. Platelet-activating Factor Receptor (PAFR) Inhibitor

    TSI-01 is a selective inhibitor of the Platelet-activating Factor Receptor (PAFR), targeting lysophosphatidylcholine acyltransferase (LPCAT)2. This compound exhibits a potent inhibitory effect with an IC50 of 0.47 μM for human LPCAT2, significantly more effective than its activity on LPCAT1 (IC50 = 3.02 μM). TSI-01 effectively suppresses PAF biosynthesis in mouse peritoneal macrophages when stimulated with a calcium ionophore at a concentration of 60 μM. This makes TSI-01 a valuable tool for investigating inflammatory processes and related conditions in research applications.
  45. PAFR Antagonist

    MK 287 is a potent and selective antagonist of the platelet-activating factor receptor (PAFR). It effectively inhibits [3H]C18-PAF binding to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes, with K1 values of 6.1, 3.2, and 5.49 nM, respectively. MK 287 also demonstrates the ability to inhibit PAF-induced platelet aggregation and elastase release from PMNs, with ED50 values of 56, 1.5, and 4.4 nM. This compound is valuable for research focused on cardiovascular diseases, including thrombosis.
  46. PAF Antagonist

    CV-6209 is a potent antagonist of platelet activating factor (PAF) that effectively inhibits PAF-induced aggregation in both rabbit and human platelets, demonstrating IC50 values of 75 nM and 170 nM, respectively. Additionally, CV-6209 has been shown to inhibit PAF-induced hypotension in rat models. This compound is valuable for research focused on platelet function, cardiovascular responses, and PAF-related pathways.
  47. PAF Agonist

    Carbamyl-PAF is an analog and agonist of platelet-activating factor (PAF). It exhibits potent biological activity by stimulating PAF receptors, which play a crucial role in mediating inflammatory responses. Due to its stability and resistance to metabolism in Raji lymphoblasts at 37°C, Carbamyl-PAF is an effective reagent for studying PAF-related signaling pathways and inflammation mechanisms.
  48. PAF Receptor Antagonist

    MoTP is a selective antagonist of the platelet-activating factor (PAF) receptor, known for its ability to induce melanocyte ablation. This compound exhibits significant biological activity that can be leveraged in cancer research, offering insights into melanocyte regulation and tumor microenvironment interactions. MoTP is a valuable reagent for studies aimed at understanding the role of PAF signaling in tumor biology and potential therapeutic strategies.
  49. Platelet-activating Factor Antagonist

    Kadsurenone is a lignan that acts as a specific antagonist of platelet-activating factor (PAF). By inhibiting PAF, Kadsurenone demonstrates potential anti-inflammatory and anti-platelet effects. This compound is commonly explored in research related to cardiovascular disorders and other conditions associated with platelet activation. Kadsurenone can be obtained from the stem of Piper kadsura, providing a natural source for studying its biological activities.
  50. Platelet Aggregation Inhibitor

    2-Acetylbenzoic acid is a derivative of benzoic acid that functions as a weak inhibitor of platelet aggregation. It specifically inhibits adenosine 5'-diphosphate (ADP)-induced platelet aggregation, making it valuable for research in cardiovascular biology and thrombotic disorders. This compound can be utilized to study the role of platelet activation in various disease models and therapeutic interventions.

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