GPCR/G Protein

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  1. Adrenergic Receptor Antagonist

    (±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist. This compound demonstrates potential to modulate adrenergic signaling pathways, making it a valuable tool in studies of cardiovascular function and neurobiology. Its ability to inhibit α2-adrenergic receptors positions it as a candidate for investigating therapeutic strategies in conditions related to adrenergic dysregulation.
  2. Adrenergic Receptor Agonist

    Dopexamine hydrochloride is a selective β2 adrenergic receptor agonist. It exhibits positive inotropic and vasodilatory effects, making it valuable in the treatment of heart failure and shock. Additionally, its ability to enhance cardiac output and tissue perfusion underpins its application in cardiovascular research and studies investigating adrenergic signaling pathways.
  3. β3-adrenergic Receptor Inhibitor

    Vemtoberant is a selective β3-adrenergic receptor inhibitor with a human Ki of 8.2 nM, demonstrating a significant selectivity of 400- to 600-fold over the human β1- and β2-adrenergic receptors. This compound effectively attenuates β3-AR-mediated cardiac inhibition, making it a valuable tool for studying mechanisms underlying systolic heart failure. Researchers can utilize Vemtoberant to investigate therapeutic strategies aimed at modulating β3-adrenergic signaling in cardiac contexts.
  4. Stable Isotope

    Propranolol-d7 is a stable isotope-labeled form of Propranolol, a nonselective β-adrenergic receptor (βAR) antagonist. It exhibits high affinity for β1AR and β2AR, with inhibition constants (Ki) of 1.8 nM and 0.8 nM, respectively. Propranolol's capability to inhibit [3H]-DHA binding to rat brain membranes, with an IC50 of 12 nM, makes it a valuable tool for researching conditions such as hypertension, myocardial infarction, cardiac arrhythmias, and other cardiovascular disorders.
  5. ADRB2 Agonist

    Mabuterol is a selective beta-2 adrenergic receptor (ADRB2) agonist with oral bioavailability. This compound inhibits cell proliferation and effectively suppresses the rise of intracellular calcium levels triggered by PDGF-BB. Additionally, Mabuterol reduces protein expression of Drp-1, cyclin D1, and PCNA, while enhancing Mfn-2 expression in response to PDGF-BB. These properties make it a valuable tool for research into cellular proliferation and signaling pathways.
  6. Isomer

    (2R)-SR59230A is the isomer of SR59230A, serving as a crucial experimental control in research settings. As a potent and selective antagonist of the β3-adrenergic receptor, it penetrates the blood-brain barrier and exhibits IC50 values of 40, 408, and 648 nM for the β3, β1, and β2 receptors, respectively. This compound is valuable for studying the pharmacological roles of β-adrenergic receptors and their implications in metabolic disorders and neurological conditions.
  7. α1-adrenergic Receptor Antagonist

    (R)-Terazosin is a potent α1-adrenergic receptor antagonist, specifically the active R-enantiomer of Terazosin. It exhibits high affinity for the α1a, α1b, and α1d subtypes with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively. This compound is primarily utilized in research applications focused on cardiovascular studies and the treatment of benign prostatic hyperplasia, offering insights into adrenergic signaling pathways and their therapeutic implications.
  8. Adrenergic Receptor Antagonist

    Dicentrine is an α1-adrenoceptor antagonist derived from the plant Stephania epigaea Lo. This natural product exhibits antihypertensive properties and has shown efficacy against human hyperplastic prostate tissues. Its selective inhibition of adrenergic receptors makes it a valuable compound for studying blood pressure regulation and benign prostatic hyperplasia in various research applications.
  9. β3-Adrenergic Receptor Agonist

    LY377604 is a selective agonist of the human β3-adrenergic receptor, exhibiting an EC50 of 2.4 nM. In addition to its agonistic activity, it antagonizes β1- and β2-adrenergic receptors. This compound is utilized in research applications related to metabolic regulation, cardiovascular studies, and the exploration of therapeutic strategies for obesity and diabetes.
  10. β-Adrenergic Receptor Agonist

    Hexoprenaline is a selective β-adrenergic receptor agonist that promotes bronchodilation through the activation of adenylate cyclase. This compound enhances the uptake of 14C-Aminopyrine and exhibits significant anti-inflammatory and anti-infective properties. Additionally, Hexoprenaline is associated with increased placental weight and improved blood flow. It serves as a valuable reagent for research in inflammation, immunology, infection, endocrinology, and neurological disorders, including asthma, chronic bronchitis, and organophosphorus compound intoxication.
  11. α2 Agonist

    Apraclonidine hydrochloride is a selective α2 adrenergic receptor agonist with weak α1 receptor activity. It is primarily used to reduce intraocular pressure (IOP) in conditions such as glaucoma by decreasing aqueous humor production. Additionally, this compound can facilitate eye lid elevation and is utilized in various ophthalmic research applications.
  12. β-AR Ligand

    CGP 12177 hydrochloride is a selective β-Adrenergic receptor (β-AR) ligand, primarily functioning as a β3-AR agonist (Ki = 88 nM) while acting as an antagonist at β1/β2-ARs (Ki = 0.9 nM for β1; Ki = 4 nM for β2). This compound also exhibits partial agonist activity for α1-AR in rat pulmonary artery. Notably, CGP 12177 hydrochloride influences the expression of uncoupling protein and leptin genes in adipose tissues of NMRI mice, making it a valuable tool for research in cardiovascular and metabolic disease mechanisms.
  13. β2-Adrenergic Receptor Agonist

    Protokylol hydrochloride serves as a potent agonist of the β2-adrenergic receptor. This compound demonstrates significant bronchodilator activity, making it valuable in research related to respiratory function and pulmonary pharmacology. Additionally, it interacts with the TRPV1 receptor, further expanding its potential applications in studying pain pathways and sensory responses.
  14. Stable Isotope

    Propranolol-d7 (ring-d7) is a deuterated analogue of Propranolol hydrochloride, a nonselective β-adrenergic receptor antagonist. It exhibits high affinity for both β1 and β2 adrenergic receptors, with Ki values of 1.8 nM and 0.8 nM, respectively. This compound inhibits [3H]-DHA binding in rat brain membranes with an IC50 of 12 nM, making it a valuable tool for studying cardiovascular conditions such as hypertension, myocardial infarction, and cardiac arrhythmias. Propranolol-d7 (ring-d7) is particularly useful in pharmacokinetic and metabolic studies using mass spectrometry due to its stable isotope labeling.
  15. β-adrenergic Receptor Antagonist

    Propranolol-d7 hydrochloride is a deuterium-labeled β-adrenergic receptor antagonist, exhibiting high affinity for both β1 and β2 adrenergic receptors with Ki values of 1.8 nM and 0.8 nM, respectively. It effectively inhibits [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is widely utilized in research focused on cardiovascular conditions such as hypertension, myocardial infarction, cardiac arrhythmias, and angina pectoris, as well as in studies on pheochromocytoma and hypertrophic cardiomyopathy.
  16. Adrenergic Blocker

    Dibenamine hydrochloride is a competitive and irreversible adrenergic blocker that modulates the effects of epinephrine by binding to adrenergic receptors. This compound has been shown to significantly enhance the rate of degradation of I-epinephrine in murine models. It is widely utilized in research applications focusing on cardiovascular pharmacology and the study of adrenergic signaling pathways.
  17. β2 Adrenoreceptor Agonist

    Procaterol hydrochloride hemihydrate is an orally active β2 adrenoreceptor agonist that primarily targets the β2 adrenergic receptors. It exhibits significant bronchodilatory activity, making it useful in studies related to asthma. This compound is valuable for researching therapeutic approaches to manage respiratory disorders and improving pulmonary function.
  18. Noradrenaline Antagonist

    (±)-WB 4101 hydrochloride is a potent antagonist of noradrenaline, primarily targeting adrenergic receptors. This compound demonstrates significant efficacy in inhibiting noradrenaline's biological activity, influencing smooth muscle function. Its applications extend to pharmacological research in cardiovascular studies and investigations involving the modulation of adrenergic signaling pathways.
  19. Active Compound

    Scopoline is an active compound that functions as an α1 adrenergic receptor agonist. It has been shown to exert significant biological activity in modulating cardiovascular responses and may play a role in various research applications related to hypertension and other adrenergic signaling pathways. This compound is valuable for studies investigating the therapeutic potential of adrenergic receptor modulation.
  20. Adrenergic Receptor Control

    3-Hydroxy xylazine is a metabolite of the α2-adrenergic receptor agonist xylazine, primarily engaging with adrenergic receptors to exert its effects. This compound is significant in the study of adrenergic signaling pathways and can be utilized in research involving sedation and analgesia. Its role as a metabolite provides insight into the pharmacokinetics and mechanism of action of xylazine in various biological systems.
  21. β2-AR Agonist

    3,4-Dihydro-6,7-isoquinolinediol acts as a selective β2-adrenergic receptor (β2-AR) agonist, exhibiting an EC50 of 106.9 μM in CH-K1/GA1S cells. In addition to its agonistic activity, it demonstrates anti-inflammatory properties by inhibiting nitric oxide production in lipopolysaccharide-stimulated mouse macrophage RAW 264.7 cells. This compound is suitable for research applications exploring β2-AR signaling and its implications in inflammation.
  22. β-block Agent

    Timolol is a non-selective β-blocker that primarily acts on β-adrenergic receptors. It is widely utilized for its ability to lower intraocular pressure in conditions such as open-angle glaucoma and ocular hypertension. Additionally, Timolol serves as a valuable research tool for studying various cardiovascular and neurological conditions, including hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation. Its cardioprotective properties further underscore its relevance in therapeutic investigations.
  23. Adrenergic Receptor Inhibitor

    Todralazine hydrochloride is a selective β2 adrenergic receptor inhibitor primarily used in the treatment of hypertension. Its mechanism involves blocking β2 adrenergic receptors, contributing to its effectiveness as an antihypertensive agent. In addition to its receptor inhibition, Todralazine hydrochloride exhibits antioxidant properties, providing potential benefits in research focused on oxidative stress and cardiovascular health.
  24. Adrenergic Receptor Agonist

    Amidephrine is a selective agonist of the alpha 1-adrenergic receptor, primarily involved in modulating smooth muscle contraction. It effectively inhibits monopulse field contraction in both the vas deferens epithelium and prostate gland, demonstrating its potential utility in studies of reproductive physiology and urology. This compound is valuable for research applications focused on adrenergic receptor signaling and its physiological implications.
  25. Stable Isotope

    Clenbuterol-d9 is a deuterium-labeled derivative of Clenbuterol, a selective β2-adrenergic receptor agonist known for its potent biological activity, with an EC50 of 31.9 nM. This stable isotope serves as a valuable tool for pharmacokinetic studies and metabolic research, enabling precise tracking of drug interactions and bioavailability in various biological systems. Clenbuterol-d9 is instrumental in advancing research on β-adrenergic signaling and its implications in respiratory and metabolic disorders.
  26. β1/β2 Adrenergic Receptor Antagonist

    4-Hydroxypropranolol hydrochloride is an active metabolite of Propranolol, functioning primarily as a β1 and β2 adrenergic receptor antagonist. This compound exhibits comparable potency to its parent drug, inhibiting β1-adrenergic receptors with a pA2 value of 8.24 and β2-adrenergic receptors with a pA2 value of 8.26. Additionally, 4-Hydroxypropranolol hydrochloride possesses intrinsic sympathomimetic activity, membrane stabilizing properties, and significant antioxidant effects, making it valuable in research related to cardiovascular diseases and stress response mechanisms.
  27. Adrenergic Receptor

    Tilisolol hydrochloride is a non-selective β-adrenergic antagonist that acts primarily on adrenergic receptors, demonstrating significant vasodilatory and hypotensive effects. This compound promotes relaxation of smooth muscle in canine coronary arteries through the opening of ATP-sensitive K+ channels and exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Additionally, tilisolol hydrochloride has been shown to reduce diastolic blood pressure in a dose-dependent manner, with a mild increase in heart rate observed in spinal cord-stimulated rats. It is widely used in cardiovascular research to study adrenergic signaling and blood pressure regulation.
  28. α1A-AR Degrader

    α1A-AR Degrader 9c is a selective, reversible degrader specifically targeting the α1A-adrenergic receptor (α1A-AR) through the proteasomal degradation pathway. It demonstrates significant biological activity, inhibiting the proliferation of PC-3 cells with an IC50 value of 6.12 μM. This compound is valuable for research applications in prostate cancer, providing insights into the therapeutic potential of α1A-AR degradation in oncology studies.
  29. Antiarrhythmic Agent

    (+)-Sotalol is the S-isomer of Sotalol, functioning primarily as a non-selective β-adrenergic receptor blocker. This antiarrhythmic agent is effective in prolonging action potential duration in isolated cardiac muscle, making it valuable in the study of cardiac rhythm disorders. Its role in various research applications includes examining mechanisms underlying arrhythmias and evaluating therapeutic strategies for heart rate regulation.
  30. Adrenergic Receptor Agonist

    Synephrine hydrochloride is an alkaloid that acts as an agonist for both α-adrenergic and β-adrenergic receptors. Derived from Citrus aurantium, this sympathomimetic compound exhibits stimulatory effects on the central nervous system and may promote weight loss through increased metabolic rate and thermogenesis. It is widely used in research applications investigating metabolic processes and the physiological effects of adrenergic stimulation.
  31. Lightening Agent

    Undecylenoyl phenylalanine is a competitive antagonist of α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptors (β-ADR), effectively inhibiting melanogenesis in melanocytes. This compound demonstrates significant potential as a skin lightening agent by reducing hyperpigmentation, thereby improving conditions such as melasma lesions and solar lentigines. Its mechanism of action makes it valuable for research in dermatological applications targeting skin pigmentation disorders.
  32. Beta-1 Receptor Full Agonist

    T-0509 is a selective full agonist of the β1 adrenergic receptor. It activates the cAMP signaling pathway, significantly enhancing myocardial contractility. This compound is useful in research applications investigating cardiac function, β1 receptor signaling, and related pharmacological effects in cardiovascular studies.
  33. Adrenergic Receptor Agonist

    Brombuterol hydrochloride is a selective β-adrenergic receptor agonist known for its ability to stimulate adenylate cyclase, leading to increased cyclic AMP levels. This compound exhibits significant bronchodilatory effects, making it useful in research related to respiratory disorders such as asthma and chronic obstructive pulmonary disease (COPD). Additionally, Brombuterol hydrochloride serves as a valuable tool in the study of adrenergic signaling pathways and their role in various physiological processes.
  34. α-adrenergic Receptor Antagonist

    (S)-Terazosin is a selective α-adrenergic receptor antagonist, exhibiting high affinity for α1a, α1b, and α1d-adrenoceptors with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, respectively. Additionally, it interacts with α2a, α2B, and α2c-adrenoceptors, showing Ki values of 729 nM, 3.5 nM, and 46.4 nM. This compound is primarily utilized in research focused on cardiovascular conditions, benign prostatic hyperplasia, and as an innovative tool in understanding adrenergic signaling pathways.
  35. Adrenergic Receptor

    Ethylnorepinephrine hydrochloride is a sympathomimetic compound that primarily targets adrenergic receptors. It exhibits bronchodilator activity, making it valuable in research focused on respiratory disorders and cardiovascular responses. This reagent is utilized in studies involving the modulation of sympathetic nervous system activity and the investigation of adrenergic signaling pathways.
  36. Stable Isotope

    Isoxsuprine-d6 hydrochloride is a deuterium-labeled form of Isoxsuprine hydrochloride, a selective beta-adrenergic receptor agonist. It exhibits inhibitory constants (Kis) of 13.65 μM and 3.48 μM for myometrial and placental beta-adrenergic receptors, respectively, and also functions as an NMDA receptor antagonist. This stable isotope variant is valuable for pharmacokinetic studies and metabolic tracing in biological research, facilitating an understanding of drug interactions and mechanisms of action.
  37. Adrenergic Receptor Agonist

    Prenalterol is a selective β1-adrenergic receptor agonist that primarily targets cardiovascular pathways. It facilitates increased cardiac contractility without affecting gastrointestinal smooth muscle activity. This compound is valuable for research applications focused on cardiovascular disease mechanisms and therapeutic interventions.
  38. Adrenergic Receptor

    (-)-Dihydroalprenolol serves as a β-adrenergic receptor antagonist, effectively inhibiting β-adrenergic receptor activity. This compound is known to induce desensitization in approximately 60% of β-adrenergic receptor binding sites and decreases the binding affinity of specific β-adrenergic ligands. Additionally, (-)-Dihydroalprenolol may influence the stimulation of membrane-bound adenylate cyclase, making it a relevant tool in cardiovascular and pharmacological research applications.
  39. α2B/2C Adrenoceptor Antagonist

    ARC 239 dihydrochloride is a selective antagonist of the α2B and α2C adrenoceptors, demonstrating pKd values of 5.95, 7.41, and 7.56 at the α2A, α2B, and α2C receptors, respectively. This compound effectively binds to CHO cell membranes expressing human recombinant α2A, α2B, and α2C adrenoceptor subtypes, showing pKi values of 5.6, 8.4, and 7.08. ARC 239 dihydrochloride is valuable for research applications in studying adrenergic signaling pathways and the physiological roles of α2 adrenergic receptors.
  40. Stable Isotope

    Bisoprolol-d5 is a deuterium-labeled derivative of Bisoprolol, a selective and potent β1-adrenergic receptor blocker. This compound predominantly inhibits β1-receptors with minimal β2-receptor activity, making it relevant for research in hypertension, coronary artery disease, and stable ventricular dysfunction. Bisoprolol-d5 serves as a valuable tool in pharmacokinetic studies and metabolic profiling.
  41. α-2C Adrenergic Receptor Antagonist

    ORM-10921 free base is a selective antagonist of the α-2C adrenergic receptor, exhibiting a Ki value of 1.4 nM. This compound demonstrates significant antidepressant and antipsychotic-like activities, making it a valuable tool for research in neuropharmacology and the exploration of mood disorders. Its specificity and potency position ORM-10921 free base as a potential candidate for studies related to the modulation of neurotransmitter systems.
  42. Stable Isotope

    Oxprenolol-d7 hydrochloride is a deuterium-labeled derivative of the β-adrenergic receptor antagonist, Oxprenolol. It exhibits a Ki of 7.10 nM in radioligand binding assays, demonstrating effective inhibition of β-AR activity. This stable isotope is primarily used in pharmacokinetic studies and metabolic research, facilitating investigations into the metabolism and distribution of β-adrenergic antagonists in biological systems.
  43. β3- Adrenergic Receptor Agonist

    Mirabegron impurity-1 is a potent and selective β3-adrenergic receptor agonist. It has been shown to inhibit metabolism, contributing to its biological activity. This compound is valuable for research applications focused on bladder function and related disorders, facilitating studies into the pharmacological effects of β3-adrenergic modulation.
  44. Deuterated Brombuterol

    Brombuterol-d9 is a deuterated form of Brombuterol, a selective β-adrenergic receptor agonist. This compound is utilized in pharmacological research to investigate β-adrenergic signaling pathways and assess the pharmacokinetics of Brombuterol in biological systems. Its deuterated nature enhances analytical sensitivity in mass spectrometry and other detection methods, making it a valuable tool for studying drug metabolism and receptor interactions.
  45. Adrenergic Receptor Antagonist

    Nadolol-d9 is a deuterated derivative of Nadolol, functioning as a non-selective antagonist of β-adrenergic receptors. By inhibiting these receptors, Nadolol-d9 plays a significant role in cardiovascular research, particularly in studies related to hypertension and arrhythmias. Its stable isotope labeling enhances metabolite tracking and pharmacokinetic profiling in drug development.
  46. Stable Isotope

    Sotalol-d6 hydrochloride is a deuterium-labeled derivative of Sotalol hydrochloride, a potent non-selective competitive β-adrenergic receptor blocker. This compound exhibits significant antiarrhythmic activity and is primarily utilized in research focused on pediatric arrhythmias. In addition to blocking β-receptors, Sotalol-d6 also inhibits potassium KCNH2 channels, providing valuable insights into cardiac electrophysiology and potential therapeutic applications.
  47. α2 Receptor Agonist

    Guanoxabenz hydrochloride is a selective α2 adrenergic receptor agonist, demonstrating a Ki value of 4000 nM and a fully activated form with a potency of 40 nM at the α2A adrenoceptor. This compound plays a crucial role in modulating adrenergic signaling pathways and is commonly utilized in research investigating autonomic regulation, anxiety disorders, and analgesic effects. Its specificity for the α2 receptors supports studies aimed at exploring therapeutic targets for various neurological conditions.
  48. β-adrenoceptor Agonist

    Arbutamine is a potent, nonselective β-adrenoceptor agonist that primarily targets β1-, β2-, and β3- adrenergic receptors. This short-acting compound enhances cardiac stress by increasing heart rate, contractility, and systolic blood pressure. Arbutamine is utilized in research applications related to cardiac function and stress testing, providing valuable insights into adrenergic receptor activity within cardiovascular studies.
  49. Stable Isotope

    Brimonidine-d4 is a deuterium-labeled derivative of Brimonidine, a potent agonist of the α2-adrenergic receptor (α2-AR). This stable isotope is primarily utilized in pharmacokinetic studies and metabolic profiling to trace and quantify Brimonidine in biological systems. Its applications extend to research involving ocular therapies and the modulation of neurotransmitter release through α2-AR pathways.
  50. α1 Adrenoceptor Antagonist

    Benoxathian hydrochloride is a potent α1 adrenoceptor antagonist primarily used in research to investigate the mechanisms of anorexia. Its action on α1 adrenergic receptors can provide insights into appetite control and related metabolic pathways, making it a valuable tool for studies in neuropharmacology and appetite regulation.

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