GPCR/G Protein

Items 5851-5900 of 6977

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  1. Endothelin Receptor Agonist

    [Lys4] Sarafotoxin S6c is a potent partial agonist of the endothelin receptor. This sarafotoxin analogue induces contraction in pig coronary artery tissues, demonstrating an EC50 of 1.5 nM. It serves as a valuable tool for research in cardiovascular physiology and the study of endothelin receptor signaling pathways.
  2. ETB Receptor Antagonist

    RES-701-1 is a cyclic peptide that serves as a specific antagonist for the endothelin receptor type B (ETB). This compound effectively inhibits the binding of 125I-labeled endothelin-1 (ET-1) to the ETB receptor, demonstrating an IC50 value of 10 nM. RES-701-1 is primarily utilized for research applications aimed at studying the role of ETB receptors in cardiovascular and other physiological processes.
  3. ETA Antagonist

    Edonentan hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, exhibiting a high affinity with a Ki value of 10 pM. This compound demonstrates 100% oral bioavailability in rat models, making it an effective tool for in vivo studies. Edonentan hydrate is primarily utilized in research focused on cardiovascular disease and other conditions where endothelin signaling is implicated.
  4. ET-A Receptor Antagonist

    JKC 302 is an endothelin-1 (ET-1) receptor type A (ET-A) antagonist that inhibits ET-1-induced contraction in asthmatic rat trachea rings. This compound serves as a valuable tool for studying the role of endothelin signaling in respiratory conditions and may aid in the development of therapeutic strategies for asthma and related disorders. Its application in research provides insights into the mechanisms underlying airway hyperreactivity and constriction.
  5. Endothelin-B Receptor Antagonist

    PD 142893 is an endothelin-B receptor antagonist that selectively inhibits the action of endothelin-1, a potent vasoconstrictor. This compound demonstrates significant biological activity in modulating blood pressure and vascular resistance, making it a valuable tool in cardiovascular research. PD 142893 is widely used to study the role of endothelin signaling in various physiological and pathological conditions, including pulmonary hypertension and heart failure.
  6. ETB Antagonist

    K-8794 is a selective endothelin receptor type B (ETB) antagonist that exhibits oral bioactivity. This compound is valuable for investigating its potential therapeutic effects in cardiovascular diseases by modulating endothelin-mediated pathways. K-8794 can aid in elucidating the role of ETB receptors in various biological processes and support research on related cardiovascular conditions.
  7. Endothelin ETA Receptor Antagonist

    S-1255 is a highly selective endothelin ETA receptor antagonist with a dissociation constant (Kd) of 0.39 nM. This compound effectively inhibits vasoconstriction, leading to sustained hypotensive effects in hypertensive animal models. S-1255 serves as a valuable tool in the study of hypertension and related cardiovascular disorders, providing insights into the endothelin signaling pathway and its role in vascular regulation.
  8. Endothelin-A Antagonist

    BMS-187308 is an orally active antagonist of the endothelin-A (ETA) receptor, exhibiting a Ki of 4.7 nM for ETA and a Ki of 1.7 μM for ETB. This compound effectively inhibits the pressor response to endothelin-1 (ET-1) with an ED25 value of 1.2 µmol/kg when administered intravenously. BMS-187308 serves as a valuable tool for research focused on the physiological and pathophysiological roles of endothelin in various biological systems.
  9. Endothelin Receptor Agonist

    Sarafotoxin S6b is a potent vasoconstrictor peptide and a non-selective agonist of endothelin receptors. This compound effectively induces contraction in isolated human coronary arteries, exhibiting Ki values of 0.27 nM, 0.55 nM, and 19.5 nM for the coronary artery, saphenous vein, and coronary artery, respectively. Sarafotoxin S6b is valuable for research applications focused on cardiovascular physiology and the roles of endothelin signaling in vascular constriction.
  10. Endothelin (ETA) Receptor Antagonist

    CI-1020 is a selective antagonist of the endothelin (ETA) receptor, exhibiting an IC50 value of 0.3 nM. This compound effectively inhibits intimal hyperplasia in human saphenous vein organ culture. Furthermore, CI-1020 demonstrates potential in the treatment of hypoxic pulmonary hypertension by blocking ET-1-induced pressor responses following oral administration, making it a valuable tool for research in vascular biology and cardiovascular diseases.
  11. Endothelin A Receptor Antagonist

    Fandosentan potassium is a selective antagonist of the endothelin A receptor (ETAR). It effectively reverses hypoxic pulmonary vasoconstriction in perinatal lamb models, making it a valuable tool for investigating pulmonary hypertension. Additionally, Fandosentan potassium inhibits the activities of CYP2C9 and CYP3A4 with IC50 values of 39.6 μM and 21.6 μM, respectively, supporting its application in exploring drug metabolism and interactions.
  12. ETB Receptor Agonist

    BQ-3020 is a selective endothelin receptor (ETB receptor) agonist known for its ability to displace [125I] ET-1 binding at ETB receptors, exhibiting an IC50 of 0.2 nM. This compound induces vasoconstriction in the rabbit pulmonary artery and promotes relaxation of the pig urinary bladder neck. BQ-3020 is valuable for research in cardiovascular diseases, providing insights into endothelin signaling pathways and their physiological implications.
  13. ETA Receptor Antagonist

    PD 155080 is a selective antagonist of the endothelin A (ETA) receptor. It effectively reduces coronary resistance in isolated rat heart models and enhances both systolic and diastolic myocardial function in ischemia/reperfusion studies. This reagent is valuable for research focused on cardiovascular diseases, including the investigation of endothelin's role in cardiac function and pathology.
  14. Endothelin converting enzyme inhibitor

    Daglutril targets the endothelin receptor, exhibiting the ability to modulate cytokine-induced endothelin-1 production in astrocytes. Its inhibitory effects on endothelin-1 generation make it a valuable research tool for screening compounds that regulate this peptide's synthesis in glial cells. This compound is particularly relevant for studies investigating the role of endothelin-1 in neuroinflammation and related neurological disorders.
  15. Endothelin Receptor Antagonist

    TAK 044 is an antagonist of the Endothelin Receptor, exhibiting potent inhibitory effects on endothelin-induced pathological changes in various animal models. This compound is valuable for exploring the role of endothelin in diseases such as acute myocardial infarction, acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage. Researchers can leverage TAK 044 to investigate therapeutic strategies targeting endothelin-related conditions.
  16. Endothelin Antagonist

    PD 156252 is a highly potent endothelin antagonist, primarily targeting the ETA and ETB receptor subtypes. It exhibits enhanced binding affinity with IC50 values of 1.0 nM for rabbit ETA receptors and 40 nM for rat ETB receptors. This compound is valuable for research applications focusing on the endothelin system, cardiovascular studies, and investigations into related pathophysiological conditions.
  17. ETA Receptor Antagonist

    BQ-610 is a selective antagonist of the endothelin A receptor (ETA), functioning as a competitive inhibitor of endothelin-1 (ET-1) binding. This inhibition leads to the attenuation of vascular smooth muscle contraction, reduction in cell mitosis, and diminished hormone secretion. BQ-610 has demonstrated efficacy in alleviating cerebral vasospasm in animal models, inhibiting bronchial epithelial and pulmonary vascular cell proliferation induced by cigarette smoke, and delaying natural luteal regression in bovine reproduction. This reagent is valuable for research focusing on vasospasm, abnormal cellular proliferation, and reproductive endocrine disorders.
  18. Macitentan Metabolite

    ACT-373898 is the inactive carboxylic acid metabolite of Macitentan, a non-peptide dual antagonist of ETA and ETB endothelin receptors. This compound serves as a valuable reference for studies examining the pharmacokinetics and metabolic pathways of Macitentan. Its characterization is essential for understanding the therapeutic efficacy and safety profiles associated with endothelin receptor modulation in cardiovascular research.
  19. Endothelin Receptor Antagonist

    TA-0201 is a competitive, non-peptide antagonist targeting endothelin receptors. It effectively inhibits the binding of [125I]ET-1 to cloned human ETA and ETB receptors, demonstrating Ki values of 15 pM and 41 nM, respectively. TA-0201 further reduces the pressor response induced by exogenous big ET-1, making it a valuable tool for studies aimed at understanding endothelin-mediated pathways and potential therapeutic interventions in cardiovascular research.
  20. Adenosine Analog

    5'-O-[Bis(4-methoxyphenyl)phenylmethyl]-adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for cancer research. It serves as a useful tool in studies focused on adenosine receptor modulation and vascular biology.
  21. Adenosine Analog

    3’-O-Propargyladenosine is an adenosine analog that primarily targets adenosine receptors, acting as a vasodilator and exhibiting potential anti-cancer properties. It serves as a valuable tool in research applications involving click chemistry, due to its alkyne functional group, which facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This compound is instrumental in the study of biochemical pathways and therapeutic interventions related to adenosine signaling and vascular biology.
  22. Adenosine Analog

    N6-Bz-5'-O-DMTr-3'-deoxyadenosine-2'-O-CED-phosphoramidite is an adenosine analog that primarily targets adenosine receptors. It exhibits biological activities such as smooth muscle relaxation and has demonstrated potential in inhibiting cancer progression. This compound is useful in various research applications, particularly in the development of nucleic acid-based therapeutics and the study of adenosine receptor signaling pathways.
  23. Adenosine Analog

    5’-O-(4,4’-Dimethoxytrityl)-2’-beta-C-methyl adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound exhibits significant biological activities, including the inhibition of cancer progression. It serves as a valuable tool in research applications related to cardiovascular research, cancer therapies, and the study of adenosine receptor signaling pathways.
  24. Adenosine Analog

    N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. This compound is valuable for research applications focusing on vascular biology, oncology, and the investigation of adenosine signaling pathways.
  25. Adenosine Analog

    N-[[4-(Trifluoromethyl)phenyl]methyl]adenosine is an adenosine analog known for its smooth muscle vasodilatory effects. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for research in oncology and cardiovascular studies. Its biological activity positions it as a key reagent for investigating adenosine receptor pathways and their implications in various therapeutic contexts.
  26. Adenosine Analog

    8-Benzyloxyadenosine is an adenosine analog that primarily targets adenosine receptors to elicit biological responses. This compound exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular biology and cancer therapeutics.
  27. Adenosine Analog

    5-Methyl-4’-thiouridine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects, promoting smooth muscle relaxation, and has shown potential in inhibiting cancer progression. Its applications in research encompass studies on cardiovascular function and cancer therapeutics.
  28. Adenosine Analog

    8-Bromo-5’-O-(4-cyanobenzyl)-2’,3’-di-O-isopropylidene adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory activity and has potential applications in cancer research due to its ability to inhibit cancer progression. Its structural modifications make it a valuable tool for studying adenosine signaling pathways in various biological systems.
  29. Adenosine Analog

    2'-O-t-Butyldimethylsilyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound functions as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It is valuable for research applications in vascular biology and oncology, contributing to studies on therapeutic pathways involving adenosine signaling.
  30. Adenosine Analog

    2-Benzylthioadenosine is an adenosine analog that primarily acts on adenosine receptors. It is known for its vasodilatory effects on smooth muscle and has been investigated for its potential to inhibit cancer progression. This compound is valuable in research applications related to cardiovascular health and oncology, contributing to the understanding of adenosine signaling pathways.
  31. Biochemical Assay Reagent

    Adenosine 2'-PEG-Biotin is a biochemical assay reagent that acts as a bioisostere of endogenous adenosine, allowing it to engage adenosine receptors effectively. This compound plays a crucial role in regulating various cell signaling pathways, facilitating research into its applications as a bioprobe, biosensor, or diagnostic reagent. Its incorporation of biotin also enhances its utility in various biochemical assays and detection methodologies.
  32. Adenosine Analog

    N6-Benzoyl-2',3'-isopropylidene adenosine is an adenosine analog targeting adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has demonstrated potential in inhibiting cancer progression. Its applications in research include studying vascular physiology and cancer biology, making it a valuable tool in the investigation of therapeutic strategies involving adenosine modulation.
  33. Adenosine Analog

    2'-O-Acetyl-3,5-bis-O-(2,4-dichlorobenzyl)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has potential applications in inhibiting cancer progression. Its mechanism of action makes it a valuable tool for researchers studying cardiovascular function and cancer therapeutics.
  34. Adenosine Analog

    5′-O-[(4-Cyanophenyl)methyl]-2′,3′-O-(1-methylethylidene)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory properties and demonstrates potential in inhibiting cancer cell proliferation. It is a valuable tool in research exploring the effects of adenosine signaling in cardiovascular diseases and cancer therapy.
  35. Adenosine Analog

    N4-Benzoyl-5'-O-DMT-2'-O-propargyl adenosine is an adenosine analog that acts primarily as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for various biological research applications. Its distinctive structural properties facilitate the study of adenosine receptor interactions and signaling pathways, contributing to the understanding of cardiovascular physiology and tumor biology.
  36. Adenosine Analog

    N6-Benzyl-2’-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory effects in smooth muscle and demonstrates potential in inhibiting cancer progression. It serves as a valuable tool in studies focusing on cardiovascular function and cancer biology, facilitating research into therapeutic strategies for related conditions.
  37. Adenosine Analog

    N-[(3-Methoxyphenyl)methyl]adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It is a valuable tool for researchers investigating vascular biology and cancer therapeutics.
  38. Uridine Analog

    5-Iodo-2’-β-C-methyl uridine is a uridine analog that primarily targets adenosine receptors. This compound exhibits potential antiepileptic properties and serves as a valuable tool in the investigation of anticonvulsant and anxiolytic activities. Additionally, it may contribute to the development of innovative antihypertensive agents in chemical research.
  39. Adenosine Analog

    5’-O-(4,4’-Dimethoxytrityl)-2’-O-(2-methoxyethyl) adenosine is an adenosine analog that primarily targets adenosine receptors. This compound demonstrates biological activities such as smooth muscle vasodilation and potential inhibition of cancer progression. It is valuable for research in cardiovascular studies and cancer biology, facilitating investigations into adenosine signaling and therapeutic applications.
  40. Adenosine Analog

    N6-Methyl-xylo-adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. Its unique properties make it a valuable tool for researchers investigating vascular biology and cancer therapies.
  41. 5'-AMP Analogue

    2-Cl-5'-AMP is a 5'-AMP analogue that functions primarily by interacting with adenosine receptors. This compound exhibits key biological activity in receptor mapping research, facilitating the study of adenosine receptor signaling pathways and their physiological roles. Its use in biochemical assays enables a deeper understanding of receptor-ligand interactions and their implications in various biological systems.
  42. Adenosine Analog

    N-Benzoyl-5'-O-dmtr-2'-O-(2-methoxyethyl)-adenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant vasodilatory effects by relaxing smooth muscle and has demonstrated potential in inhibiting cancer progression. This compound is valuable in biomedical research, particularly in studies focused on cardiovascular health and cancer therapy.
  43. Adenosine Analog

    9-(β-D-Xylofuranosyl)adenine is an adenosine analog that primarily acts as a vasodilator by targeting adenosine receptors. This compound has demonstrated significant biological activity, including the inhibition of cancer progression. It is particularly useful for researchers exploring the mechanisms of vasodilation and the therapeutic potential of adenosine-related pathways in cancer biology.
  44. Adenosine Analog

    2'-O-Methyladenosine 5'-monophosphate triethylammonium is an adenosine analog that primarily targets adenosine receptors. It exhibits significant biological activity, functioning as a smooth muscle vasodilator while also demonstrating potential for inhibiting cancer progression. This compound is valuable for research applications focusing on cardiovascular studies and cancer biology.
  45. Adenosine Analog

    8-Chloro-2'-deoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a potential vasodilator and has demonstrated inhibitory effects on cancer progression. It is useful in various research applications, particularly in studying the pharmacological effects of adenosine and its derivatives in cardiovascular and oncology research.
  46. Adenosine Analog

    2-Methoxy-2'-deoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory effects on smooth muscle and has demonstrated potential in inhibiting cancer progression, making it relevant for various research applications, including cardiovascular studies and oncology. Its structural similarity to adenosine allows for exploration in drug development targeting related pathways.
  47. Adenosine Analog

    N-(2-Phenoxyacetyl)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool in cancer research and studies related to vascular biology.
  48. Adenosine Analog

    N6-Benzoyl-9-β-D-arabinofuranosyladenine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and demonstrates potential in inhibiting cancer progression. It serves as a valuable tool in studies focused on cardiovascular research and oncology, enabling researchers to explore the therapeutic implications of adenosine signaling pathways.
  49. Adenosine Analog

    8-Allylthioadenosine is an adenosine analog that primarily targets adenosine receptors. It demonstrates smooth muscle vasodilatory effects and has been implicated in inhibiting cancer progression, making it a valuable compound for oncology research. Its utility extends to studies involving vascular biology and the modulation of cellular signaling pathways.
  50. Adenosine Analog

    3’-O-(2-Methoxyethyl)-2-aminoadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory properties and has demonstrated potential in inhibiting cancer progression. Research applications include studying vascular biology, exploring therapeutic avenues in oncology, and investigating the signaling pathways mediated by adenosine receptors.

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