GPCR/G Protein

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Product Name
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  1. CXCR4 Antagonist

    TC14012 is a peptidomimetic antagonist targeting the chemokine receptor CXCR4, exhibiting a high level of selectivity with an IC50 of 19.3 nM. In addition, TC14012 acts as a potent agonist for CXCR7, demonstrating an EC50 of 350 nM in β-arrestin 2 recruitment assays. This compound is utilized in research focused on HIV and cancer therapy, showcasing its potential in modulating chemokine signaling pathways.
  2. CXCR4 Antagonist

    FC131 TFA is a potent CXCR4 antagonist that effectively inhibits the binding of [125I]-SDF-1 to CXCR4, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-HIV activity, making it a valuable tool for research in HIV treatment and other CXCR4-related studies. Its ability to disrupt CXCR4 signaling can be explored in various biological contexts, including cancer metastasis and immune response regulation.
  3. CXCR4 Antagonist

    AMD 3465 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of both the 12G5 monoclonal antibody and CXCL12AF647 to CXCR4, demonstrating IC50 values of 0.75 nM and 18 nM in SupT1 cells, respectively. Additionally, AMD 3465 significantly impedes the replication of X4-tropic HIV strains, with IC50 values ranging from 1 to 10 nM, while showing no activity against CCR5-using (R5) viruses. This compound is suitable for research applications focusing on HIV treatment and CXCR4-related signaling pathways.
  4. HIV Inhibitor

    Schisantherin D is a dibenzocyclooctadiene lignan that exhibits significant anti-HIV activity with an EC50 of 0.5 μg/mL. This compound selectively inhibits endothelin receptor B (ETBR) and demonstrates hepatoprotective properties. Schisantherin D is valuable for research applications focused on HIV replication and the exploration of liver protective mechanisms.
  5. CXCR4 Antagonist

    KRH-3955 hydrochloride is a potent CXCR4 antagonist that effectively inhibits the binding of SDF-1α to CXCR4 with an IC50 of 0.61 nM. This compound demonstrates strong selectivity and efficacy against X4 HIV-1, with an EC50 ranging from 0.3 to 1.0 nM. KRH-3955 hydrochloride is suitable for research applications focused on HIV-1 pathogenesis and CXCR4-related signaling pathways.
  6. CXCR4 Antagonist

    FC131 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. Due to its mechanism of action, FC131 demonstrates significant anti-HIV activity, making it a valuable tool for research into HIV pathogenesis and potential therapeutic interventions.
  7. Stable Isotope

    Plerixafor-d4 is a deuterated derivative of Plerixafor, a selective antagonist of the CXCR4 receptor with an IC50 of 44 nM. This compound serves as an immunostimulant and is known for its ability to mobilize hematopoietic stem cells (HSCs). Additionally, Plerixafor has demonstrated efficacy in inhibiting HIV-1 and HIV-2 replication, with an EC50 ranging from 1 to 10 nM. Plerixafor-d4 is useful in research applications requiring stable isotopes for tracking and quantification purposes.
  8. HIV-1 Entry Inhibitor

    RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies.
  9. CXCR4 Antagonist

    CXCR4 antagonist 7 is a potent CXCR4 antagonist with an IC50 of 9.3 nM. It effectively inhibits CXCR4 receptor activity, making it a valuable tool in the investigation of HIV infection, inflammatory diseases, cancer, and WHIM syndrome. This compound provides essential insights into the roles of CXCR4 signaling in various pathological conditions.
  10. CXCR Inhibitor

    AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development.
  11. CXCR4 Antagonist

    CXCR4 Antagonist 4 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 of 24 nM. It demonstrates enhanced permeability as assessed by PAMPA and has reduced activity on CYP 2D6. This compound is particularly effective in inhibiting the entry of human immunodeficiency virus, with an IC50 value of 7 nM, making it a valuable tool for research in virology and therapeutic development targeting CXCR4-mediated pathways.
  12. CXCR Antagonist

    GSK812397 is a potent CXCR4 antagonist that functions by inhibiting the CXC chemokine receptor 4, a critical co-receptor for HIV-1 entry into host cells. This compound has demonstrated significant biological activity, making it a promising candidate for HIV treatment research. Its ability to suppress the replication of various late cytopathic viruses marks GSK812397 as a valuable reagent in the development of innovative anti-HIV therapies. Additionally, scalable synthetic routes enable efficient production, ensuring sufficient quantities for comprehensive investigation.
  13. CXCR Antagonist

    CXCR4 antagonist 1 is a selective antagonist of the chemokine receptor CXCR4. It exhibits significant anti-HIV activity by inhibiting the interaction of CXCR4 with its ligands, thereby blocking viral entry into host cells. This compound is valuable in research focused on HIV pathogenesis and the development of therapeutic strategies targeting CXCR4.
  14. CXCR4 Antagonist

    HF50731 is a potent antagonist of CXCR4, demonstrating a binding affinity with an IC50 value of 19.8 nM. This compound effectively inhibits key biological processes such as calcium mobilization and cell migration, with IC50 values of 119.2 nM and 621.4 nM, respectively. Additionally, HF50731 demonstrates the ability to inhibit HIV-1 infection through CXCR4 coreceptor blockade, achieving an IC50 of 1.5 μM. HF50731 is valuable for research in immunology, virology, and cancer biology focused on CXCR4 signaling pathways.
  15. CXCR Inhibitor

    AMD-3329 is a selective CXCR4 inhibitor that targets the chemokine receptor involved in HIV-1 and HIV-2 entry into host cells. By obstructing CXCR4, AMD-3329 effectively inhibits viral replication, making it a valuable tool in HIV research. This compound is suitable for studies focused on developing therapeutic strategies against X4-tropic HIV strains and understanding the mechanisms of viral entry and infection.
  16. Platelet-Activating Factor Antagonist

    Acopafant is a potent platelet-activating factor antagonist that plays a critical role in modulating inflammatory responses. Its ability to inhibit human immunodeficiency virus (HIV) expression in chronically infected cells highlights its potential utility in HIV research. Acopafant is valuable for studies investigating the mechanisms of HIV infection and the development of therapeutics targeting viral latency and reactivation.
  17. HIV Inhibitor

    KRH-3955 is a potent CXCR4 antagonist that demonstrates significant anti-HIV-1 activity, particularly against X4 strains. It effectively inhibits the replication of various X4 HIV-1 clinical isolates and is active against recombinant strains with resistance mutations in reverse transcriptase, protease, and tyrosinase. KRH-3955 disrupts the binding of SDF-1alpha to CXCR4, thereby interfering with calcium signaling through this receptor, along with inhibiting antibody binding to CXCR4. With an oral bioavailability of 25.6% in rats, KRH-3955 has shown efficacy in vivo, making it a valuable tool for HIV research.
  18. PAFR Antagonist

    (Rac)-Modipafant is a selective, long-acting irreversible antagonist of the platelet activating factor receptor (PAFR). This compound demonstrates significant biological activity by effectively inhibiting PAFR-mediated pathways, which plays a critical role in regulating inflammatory responses. Research applications include the investigation of dengue virus infection mechanisms and the potential therapeutic effects of PAFR blockade in various inflammatory diseases.
  19. Adenosine Receptor Antagonist

    Swertisin is an adenosine A1 receptor antagonist with additional SGLT2 inhibitory activity. This compound exhibits various biological functions, including anti-diabetic and antioxidant properties, as well as the ability to inhibit hepatitis B virus (HBV). Research has demonstrated that Swertisin can enhance cognitive function and alleviate memory impairments in murine models, making it a valuable tool for studies in diabetes, neuroprotection, and viral infections.
  20. Stable Isotope

    Rimonabant-d10 hydrochloride is a deuterium-labeled derivative of Rimonabant hydrochloride, a selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound is utilized in studies investigating the role of CB1 receptors in various physiological processes and the development of obesity therapies. Additionally, Rimonabant hydrochloride is known to inhibit Mycobacterial membrane protein Large 3 (MMPL3), making it relevant for research in tuberculosis and related infectious diseases.
  21. Dopamine β-hydroxylase Inhibitor

    A32390A is a potent inhibitor of dopamine β-hydroxylase, functioning primarily to decrease norepinephrine synthesis. This reduction can lead to lowered blood pressure, making A32390A valuable in studies related to hypertension, particularly in models such as DOCA hypertensive rats. Additionally, the compound's properties as a copper chelator allow for exploration in the context of bacterial infections and metabolic disorders, providing versatile applications in chemical research.
  22. Fungal Metabolite

    BE 24566B is a polyketide fungal metabolite that acts as an endothelin receptor antagonist, targeting both ETA and ETB receptors with IC50 values of 11 μM and 3.9 μM, respectively. This compound demonstrates antibacterial activity against a range of Gram-positive bacteria, including B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus, with reported MICs of 1.56 μg/mL for five of these species and 3.13 μg/mL for E. faecalis and S. thermophilus. BE 24566B is valuable for research applications in antimicrobial studies and receptor pharmacology.
  23. AChE/Dopamine 2 Inhibitor

    Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies.
  24. Phytocannabinoid Derivative

    Cannabigerol diacetate is a phytocannabinoid derivative that modulates cannabinoid receptors in the endocannabinoid system. This compound exhibits potential anti-inflammatory and neuroprotective activities, making it an important tool for studying the therapeutic effects of cannabinoids. Its unique structural properties also allow for exploration in various research applications, including pain management and the effects of cannabinoids on neurological disorders.
  25. Cannabinoid Derivative

    CH-FUBIATA is a synthetic cannabinoid derivative with a specific affinity for cannabinoid receptors. This compound demonstrates significant biological activity, impacting pathways involved in pain modulation, appetite regulation, and neuroprotection. CH-FUBIATA is applicable in research focusing on endocannabinoid system modulation, toxicological assessments, and the therapeutic potential of cannabinoids in various diseases.
  26. cannabinoid

    Bzo-poxizid is a synthetic cannabinoid that primarily targets cannabinoid receptors in the central nervous system. This compound exhibits psychoactive properties, making it relevant for studies investigating endocannabinoid modulation and its effects on behavior. Bzo-poxizid may also be utilized in research applications focused on the therapeutic potential of cannabinoids in various neurological disorders.
  27. Cannabinoids Precursor

    2-(2-Chlorophenyl)-1-(1H-indol-3-yl)ethanone is a key precursor in the synthesis of synthetic cannabinoids. This compound plays an essential role in the development of novel cannabinoid derivatives that may be used in pharmacological research. Its ability to modify cannabinoid structures makes it valuable for studies examining cannabinoid receptor interactions and their physiological effects.
  28. Cannabinoid-type Compounds

    (±)-9-Nor-9α-hydroxy Hexahydrocannabinol is a cannabinoid-type compound that demonstrates significant cannabinoid-like activity in animal models, specifically in dogs and mice. This compound may be of interest for research exploring the therapeutic effects and pharmacological mechanisms of cannabinoids. Its efficacy in modulating cannabinoid receptors makes it a valuable tool for studies in areas such as pain relief, anxiety reduction, and other neuropsychopharmacological applications.
  29. Phytocannabinoid Metabolite

    5'-Hydroxy-9(R)-hexahydrocannabinol is a phytocannabinoid metabolite that serves as a significant derivative of cannabinoids. It is known to exhibit potential psychoactive properties and interact with the endocannabinoid system. This compound may be utilized in research related to neuropharmacology, cannabinoid receptor studies, and the investigation of cannabis metabolites in biological systems.
  30. CB2 Receptor Ligand

    Δ8-THC methyl ether is a selective ligand for the CB2 receptor, exhibiting a favorable docking score of -10.167 kcal/mol. This compound demonstrates significant antinociceptive activity in murine models, highlighting its potential for research in pain management and cannabinoid receptor studies. Further investigation into its pharmacological properties may support its application in the development of therapeutics targeting the endocannabinoid system.
  31. Cannabinoid Derivative

    2-Fluoro QMPSB is a cannabinoid derivative that acts as a selective modulator of the cannabinoid receptors. This compound exhibits potent biological activity, making it useful for studying cannabinoid receptor mechanisms in research applications related to neuropharmacology and therapeutic developments. Its structural similarity to established synthetic cannabinoids provides valuable insights into cannabinoid receptor interactions and signaling pathways.
  32. Oxopyridine Carboxamide

    CHO-4′Me-5′Br-FUBOXPYRA is an oxopyridine carboxamide that interacts with cannabinoid receptors CB1 and CB2. This compound exhibits limited activation potential, making it a valuable tool for studying the pharmacological properties of synthetic cannabinoids. Its unique structural features support research applications in cannabinoid receptor signaling and the development of cannabinoid-related therapies.
  33. Phytocannabinoid Derivative

    (±)-9α-Hydroxy hexahydrocannabinol is a phytocannabinoid derivative that exhibits interactions with cannabinoid receptors in the endocannabinoid system. This compound has been explored for its potential therapeutic effects, including analgesic and anti-inflammatory properties. It serves as a valuable tool in research focused on understanding the pharmacological profiles of cannabinoids and their effects on various biological pathways.
  34. CB2 Receptor Agonist

    PF-03550096 is an orally active synthetic cannabinoid that selectively targets peripheral CB2 receptors, exhibiting a Ki value of 7.9 nM. This compound demonstrates notable analgesic activity, making it useful for research applications related to pain modulation and inflammation. Its selective action on CB2 receptors enhances its potential for studying cannabinoid-based therapies in various physiological contexts.
  35. Cannabinoid Derivative

    Afubiata is a cannabinoid derivative that interacts with the cannabinoid receptors in the endocannabinoid system. This compound exhibits potential biological activity related to modulating pain, inflammation, and neuroprotection. Afubiata is suitable for research applications focused on cannabinoid receptor mechanisms and the therapeutic effects of cannabinoids in various physiological processes.
  36. Phytocannabinoid Derivative

    8(S)-Hydroxy-9(R)-hexahydrocannabinol is a phytocannabinoid derivative with a unique structural profile resembling known cannabinoids. This compound exhibits significant biological activity, including potential interaction with cannabinoid receptors, which makes it a valuable tool in cannabis research. It is applicable in studies investigating the therapeutic effects of cannabinoids, including pain relief and anti-inflammatory properties.
  37. Cannabinoid Derivative

    (±)-9-Nor-9β-hydroxy Hexahydrocannabinol is a cannabinoid derivative that exhibits pronounced binding affinity for cannabinoid receptors. This compound is utilized in research to investigate the pharmacological effects of cannabinoids, including their influence on pain perception, appetite regulation, and neuroprotection. Its structural similarity to known synthetic cannabinoids makes it a valuable tool for studies focused on cannabinoid interactions and therapeutic potential.
  38. Cannabinoid Derivative

    NAPIE is a cannabinoid derivative that modulates cannabinoid receptors. It exhibits significant biological activity in the endocannabinoid system, which is pivotal for studying the therapeutic potential of cannabinoids. NAPIE is primarily used in research applications related to neurobiology, pain management, and the exploration of cannabinoid signaling pathways. Its structural similarity to existing synthetic cannabinoids makes it a valuable tool for further investigations in cannabinoid biology.
  39. Cannabinoid Derivative

    2-(1-(4-Fluorobenzyl)-1H-indol-3-yl)acetic acid is a cannabinoid derivative that interacts with cannabinoid receptors in the endocannabinoid system. This compound exhibits analgesic and anti-inflammatory properties, making it valuable for research in pain management and inflammation pathways. It serves as a useful tool in studying the pharmacological effects of cannabinoid-like substances.
  40. CB1/CB2 Agonist

    PSB-SB1202 is a phenyl coumarin compound that acts as a dual agonist for the cannabinoid receptors CB1 and CB2. It demonstrates high biological activity with EC50 values of 56 nM for CB1 and 14 nM for CB2, alongside Ki values of 32 nM and 49 nM, respectively. This compound is suitable for research applications focused on the endocannabinoid system and its implications in various physiological processes.
  41. Δ9,11-THC Analogue

    exo-Tetrahydrocannabivarin is a Δ9,11-THC analogue that demonstrates weak binding affinity for cannabinoid receptors (CB) with an IC50 of 1.4 μM. Its biological activity includes effects on motor functions and analgesia, as evidenced in preclinical models using mice. This compound is valuable for research investigating cannabinoid receptor interactions and their implications in pain management and motor control studies.
  42. Cannabinoid Receptor Antagonist

    Giminabant is a cannabinoid receptor antagonist that primarily targets CB1 receptors. It has been shown to modulate endocannabinoid signaling, making it a useful compound for studying metabolic diseases and addiction-related disorders. Its application in research may provide insights into therapeutic approaches for obesity and substance dependence.
  43. Phytocannabinoid Derivative

    Δ8-THCPA-A is a derivative of Δ8-Tetrahydrocannabiphorolic acid, designed to modulate cannabinoid receptors due to its structural similarities to known phytocannabinoids. This compound exhibits significant biological activity, contributing to research on the endocannabinoid system and its implications in therapeutic applications. It serves as a valuable tool for exploring the pharmacological effects and potential medicinal uses of cannabinoids in various biomedical studies.
  44. Phytocannabinoid Metabolite

    Carmagerol is a phytocannabinoid metabolite that interacts with the endocannabinoid system, primarily influencing cannabinoid receptor activity. It exhibits potential neuroprotective and anti-inflammatory properties, making it a valuable compound for research into its effects on pain management and neurological disorders. Carmagerol can be utilized in studies investigating the therapeutic applications of cannabinoids and their metabolites in various biological models.
  45. Phytocannabinoid Derivative

    8(R)-Hydroxy-9(R)-hexahydrocannabinol is a phytocannabinoid derivative that acts as a metabolite of 9(R)-Hexahydrocannabinol. This compound exhibits notable biological activities related to cannabinoid receptor modulation, which may be relevant for studies on cannabinoid pharmacology. It is primarily utilized in research focusing on the therapeutic potential of cannabinoids in various physiological and pathological processes.
  46. Phytocannabinoid Metabolite

    (±)-8'-Hydroxy cannabichromene is a phytocannabinoid metabolite that acts on the endocannabinoid system. It exhibits potential biological activity by interacting with cannabinoid receptors, which may influence various physiological processes. This compound is primarily utilized in research applications focused on cannabis pharmacology, cannabinoid receptor signaling, and the therapeutic effects of cannabinoids.
  47. Cannabinoid Derivative

    5-Fluoro PB-22 N-(2-fluoropentyl) isomer is a synthetic cannabinoid derivative that selectively targets cannabinoid receptors. This compound exhibits potent agonistic activity, making it valuable for research into cannabinoid receptor signaling pathways and their physiological effects. Its unique structure allows for the exploration of cannabinoid-related research applications, including studies related to neuropharmacology and the endocannabinoid system.
  48. Phytocannabinoid

    Tetrahydrocannabiphorol (THCP) is a phytocannabinoid that exhibits potent binding affinity for cannabinoid receptors, specifically CB1 and CB2. This compound has been shown to possess significant analgesic and anti-inflammatory properties, making it a valuable tool for researching pain management and therapeutic applications related to cannabinoid signaling pathways. THCP is of interest in studies examining the efficacy of cannabinoids in various health conditions and may offer insights into the pharmacological potential of cannabis-derived compounds.
  49. CB1 Agonist

    AM11542 is a selective orthosteric agonist of cannabinoid receptor 1 (CB1), exhibiting a reported binding affinity (Ki) of 0.11 nM. This compound facilitates the study of CB1 receptor activation and provides insights into the mechanisms of allosteric modulation. Its application is valuable in exploring the physiological roles of CB1 in various biological pathways and potential therapeutic targets in cannabinoid research.
  50. Biochemical Reagent

    CH-PIATA is a synthetic cannabinoid characterized by an acetamide linker, serving as a biochemical reagent in research applications. This compound exhibits potential biological activity, with EC50 values of >71 nM and >176 nM for cannabinoid receptors CB1 and CB2, respectively. CH-PIATA can be effectively detected as a parent substance in biological samples, making it a useful tool for studying cannabinoid receptor interactions and their physiological roles.

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