Catalog No.
Product Name
Application
Product Information
Citations
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MRGPRX1 PAM
MRGPRX1 agonist 3 is a potent positive allosteric modulator of the Mas-related G protein-coupled receptor X1 (MRGPRX1), exhibiting an EC50 value of 0.22 μM. This compound is instrumental in the study of neuropathic pain, facilitating investigations into the modulation of pain pathways via MRGPRX1 activation. Its unique mechanism of action makes it a valuable tool for understanding the therapeutic potential of MRGPRX1 in pain management. -
Mas-related G-protein-coupled Receptor (MRGPR) Agonist
EP-3945 is a selective agonist of the Mas-related G protein-coupled receptor (MRGPR), demonstrating greater efficacy compared to β-Alanine. This receptor is significantly involved in mediating inflammatory pruritus and pain responses. EP-3945 specifically activates the Gq signaling pathway, with an EC50 value of 211.6 nM, enabling its application in studies focused on pain modulation and itch sensation research. -
MRGPR Antagonist
Setomagpran is a selective antagonist of the mas-related G protein-coupled receptor (MRGPR). This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for investigating pathways associated with inflammation and pain. Its ability to modulate MRGPR signaling further supports research into therapeutic strategies for related disorders. -
MrgprX2 Antagonist
(R)-MrgprX2 antagonist-3 is a selective antagonist of the MrgprX2 receptor, recognized for its role in nociception and inflammatory responses. It exhibits significant potential in modulating pain and inflammation, making it a valuable tool for researching inflammatory skin disorders. This compound facilitates the exploration of therapeutic strategies aimed at targeting MrgprX2-related pathways. -
MRGPRX1 Agonist
4-Aminobenzimidamide Hydrochloride serves as a selective agonist for the Mas-related G protein-coupled receptor member X1 (MRGPRX1). This compound is instrumental in researching the signaling pathways involved in MRGPRX1-mediated analgesic effects. Its functional role in headache relief and pain modulation makes it a valuable tool for pharmacological studies focused on nociceptive pathways and pain management therapies. -
GPR142 Agonist
LY3325656 is a selective agonist of the GPR142 receptor, functioning primarily to enhance glucose-dependent insulin secretion. This compound demonstrates potential anti-diabetic effects, making it a valuable tool for research in type 2 diabetes. Its specificity for GPR142 allows for the exploration of pathways involved in insulin regulation and glucose metabolism. -
MCHR1 (GPR24) Antagonist
AZD1979 is a potent antagonist of the Melanin-concentrating hormone receptor 1 (MCHR1), exhibiting an IC50 of approximately 12 nM. This compound is primarily utilized in research aimed at understanding the physiological roles of MCHR1 in metabolic regulation and appetite control. Its antagonistic properties make it a valuable tool for studying the involvement of this receptor in various neurological and metabolic disorders. -
MCHR1 (GPR24) Agonist
Melanin Concentrating Hormone, salmon is a 19-amino-acid neuropeptide that acts as an agonist for MCHR1 (GPR24). This peptide plays a crucial role in regulating vital physiological functions such as food intake, energy balance, sleep regulation, and cardiovascular activity. Its interaction with the G protein-coupled receptor makes it a valuable tool for studying these biological pathways and investigating potential therapeutic targets related to metabolic and sleep disorders. -
MCHR1 (GPR24) Antagonist
Neuropeptide EI (rat) serves as an antagonist of the melanin-concentrating hormone receptor 1 (MCHR1, also known as GPR24). It displays functional activity by antagonizing MCH and exhibiting agonistic properties towards melanocyte-stimulating hormone (MSH). This compound is useful in research applications focused on neuropeptide signaling, metabolism, and behaviors related to feeding and energy balance. -
MCHR1 (GPR24) Antagonist
MCHR1 antagonist 1 is a selective antagonist of the melanin-concentrating hormone 1 (MCHR1) receptor, exhibiting a Kb of 1 nM and a Ki of 4 nM at human MCHR1. This compound effectively modulates the signaling pathways associated with MCHR1, making it a valuable tool in obesity research and studies focused on body weight regulation. Its specificity provides insights into the physiological roles of MCHR1 in metabolic processes. -
GPR38 Agonist
DS-3801b is a potent non-macrolide agonist of the GPR38 receptor. It demonstrates significant biological activity as a gastrointestinal prokinetic agent, making it a valuable tool for the study of functional gastrointestinal disorders such as gastroparesis and chronic constipation. Research applications of DS-3801b include the exploration of therapeutic strategies that address impaired gastrointestinal motility. -
GPR7 Antagonist
CYM 50769 is a selective antagonist of the neuropeptides B and W receptor 1 (NPBWR1). This compound has been shown to inhibit NPW-23-induced cell proliferation in ATDC5 cells, providing valuable insights into its biological activity. CYM 50769 is utilized in research focused on endochondral bone formation, enabling investigation into the roles of neuropeptides in skeletal development and related disorders. -
Gpr35 Modulator
Gpr35 Modulator 3 is a selective modulator of the Gpr35 receptor, exhibiting an IC50 of less than 1 μM. This compound is valuable for investigating its role in various biological processes, including cell proliferation, immune responses, and inflammation. Researchers can utilize Gpr35 Modulator 3 to explore the receptor's implications in related diseases and potential therapeutic applications. -
GPR52 Modulator
GPR52 agonist-4 is a selective modulator of the G-protein-coupled receptor GPR52. It demonstrates significant biological activity relevant to neuropsychiatric disorders, making it a valuable tool for research in this area. The compound's selective action on GPR52 provides insights into potential therapeutic pathways for the treatment of neuropsychiatric diseases. -
GPR52 Agonist
PW0729 is an agonist of the orphan GPR52 receptor, engaging in mechanisms that may influence neural signaling pathways. This compound shows potential in research focused on neuropsychiatric and neurological disorders through GPR52 activation and signaling bias. Further optimization of its brain exposure characteristics is needed to fully explore its therapeutic applications. -
GPR55 Agonist
O-1602 is a potent agonist of GPR55, a G protein-coupled receptor involved in various neuroinflammatory processes. It has been shown to reduce both the number and activation of hippocampal microglia triggered by methamphetamine exposure. Additionally, O-1602 decreases the expression of key proteins associated with the NLRP3 inflammasome, including NLRP3, ASC, and Caspase-1, making it a valuable tool for studies related to neuroinflammation and neurodegenerative disease research. -
GPR55 Agonist
ML-184 is a selective agonist for the GPR55 receptor, exhibiting an EC50 value of 250 nM and demonstrating over 100-fold selectivity for GPR55 compared to GPR35, CB1, and CB2. This compound triggers phosphorylation of ERK1/2 and facilitates the translocation of PKCβII to the plasma membrane through GPR55 activation. Additionally, ML-184 enhances the proliferation of neural stem cells and promotes neuronal differentiation in vitro, making it a valuable tool for research in neurobiology and cellular signaling pathways. -
GPR55 Ligand
L-α-lysophosphatidylinositol (Soy) sodium is a potent endogenous ligand for the GPR55 receptor. As a lysophospholipid and endocannabinoid neurotransmitter, it plays a crucial role in various signaling pathways. It is primarily utilized in research applications focusing on cannabinoid receptor modulation, cell signaling processes, and neurobiology studies. -
GPR55 Agonist
GPR55 Agonist 4 is a potent agonist for the G protein-coupled receptor GPR55, exhibiting an EC50 of 131 nM for human GPR55 and 1.41 nM for rat GPR55. This compound effectively induces β-arrestin recruitment, making it a valuable tool for studying GPR55 signaling pathways and its biological implications. It serves as a useful reagent in various research applications focused on neurobiology, metabolism, and inflammation. -
GPR55 Agonist
GPR55 agonist 3 is a selective agonist for the GPR55 receptor, exhibiting an EC50 of 0.239 nM for human GPR55 and 1.76 nM for rat GPR55. This compound functions by inducing β-arrestin recruitment to human GPR55 with an EC50 of 6.2 nM, facilitating various signaling pathways associated with this receptor. GPR55 agonist 3 is valuable for research applications in exploring the physiological roles and therapeutic potential of the GPR55 signaling axis. -
GPR55 Antagonist
KLS-13019 is an orally active antagonist of the GPR55 receptor, structurally related to cannabidiol (CBD). This compound has demonstrated the ability to prevent and reverse chemotherapy-induced peripheral neuropathy (CIPN) in a dose-dependent manner in rat models. Its selectivity for GPR55 makes it a valuable tool for investigating the role of this receptor in neuropathic pain and related therapeutic applications. -
GPR55 Agonist
CID1792197 is a potent agonist of the GPR55 receptor, exhibiting an EC50 value of 0.11 μM. This compound is useful in research applications focused on understanding the role of GPR55 in various pathological processes, including inflammation and pain modulation. Its ability to activate GPR55 makes it a valuable tool for exploring the therapeutic potential of this receptor in cannabinoid signaling pathways. -
GPR55 Ligand
GSK494581A is a selective ligand for the human GPR55 receptor, exhibiting a pEC50 value of 6.8, and serves as an inhibitor of glycine transporter subtype 1 (GlyT1). This compound is implicated in various biological processes, including the modulation of pain signaling, promotion of bone morphogenesis, and enhancement of vascular endothelial cell formation through its action on GPR55. Its specificity and dual activity make GSK494581A a valuable tool for research in pain management and vascular biology. -
GPR55 Agonist
CID1172084 is a selective agonist of the GPR55 receptor, exhibiting an EC50 value of 0.16 μM. This compound demonstrates over 100-fold selectivity for GPR55 compared to GPR35, CB1, and CB2 receptors. CID1172084 serves as a valuable tool for investigating the biological functions and signaling pathways associated with GPR55, facilitating research in various applications including pharmacology and neurobiology. -
GPR6 Inverse Agonist
Solangepras is a selective inverse agonist of GPR6, exhibiting a Ki of 9.4 nM and an EC50 of 38 nM. This compound is capable of penetrating the blood-brain barrier, making it a valuable tool for investigating the role of GPR6 in neurological conditions. Solangepras holds potential for advancing research in Parkinson's disease and related disorders. -
GPR6 Modulator
(S)-CVN424 is a potent modulator of G-Protein-Coupled Receptor 6 (GPR6), involved in various signaling pathways in the nervous system. This compound shows promise in the investigation of neurological and psychiatric disorders, particularly in the context of Parkinson's disease. Its ability to selectively target GPR6 makes it a valuable tool for research aimed at understanding the underlying mechanisms of these conditions. -
GPR6 Inverse Agonist
GPR6 inverse agonist 2 is a selective inverse agonist targeting the GPR6 receptor, exhibiting an IC50 of less than 0.1 μM. This compound shows notable selectivity over GPR3, with IC50 values ranging from 1 to 30 μM, and demonstrates preliminary cardiac safety with an IC50 of 21.71 μM for hERG. GPR6 inverse agonist 2 is suitable for research applications investigating movement disorders, including Parkinson's disease, offering valuable insights into therapeutic avenues for these conditions. -
GPR6 Inverse Agonist
GPR6 inverse agonist 1 is a selective inverse agonist for the GPR6 receptor, demonstrating an IC50 of less than 100 nM. This compound is essential for research investigating the pathological mechanisms of neurodegenerative disorders, particularly Parkinson's disease and Huntington's disease. Its ability to modulate GPR6 activity makes it a valuable tool for studying these conditions and exploring potential therapeutic strategies. -
GPR65 Agonist
MLS001006105 is an allosteric agonist of GPR65, demonstrating significant activity at pH 8.40. This compound is valuable for research applications focusing on the modulation of GPR65 signaling pathways, particularly in acidic microenvironments. Its unique pH-dependent mechanism offers insights into the role of GPR65 in various physiological conditions and disease states. -
GPR68 Positive Allosteric Modulator
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). This compound exhibits high selectivity for GPR68, minimizing off-target effects on related proton GPCRs, neurotransmitter transporters, and hERG ion channels. Additionally, MS48107 demonstrates the ability to effectively cross the blood-brain barrier in murine models, making it a valuable tool for neurobiological research and studies involving GPR68-related pathways. -
GPR84 Antagonist
GLPG1205 is a potent and selective antagonist of GPR84, a G-protein-coupled receptor implicated in various inflammatory processes. This compound demonstrates anti-inflammatory activity and is being investigated for its potential in treating pulmonary fibrosis. Additionally, GLPG1205 features an alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds. -
GPR84 Agonist
LY237 is an efficacious agonist of the G protein-coupled receptor GPR84, exhibiting a high potency with a pEC50 of 10.15. This compound is important for investigating the roles of GPR84 in various biological processes, particularly in the context of inflammation and fibrosis. Its activation of GPR84 may provide valuable insights into therapeutic strategies for related diseases. -
GPR84 Antagonist
GPR84 Antagonist 10 is a potent and orally bioavailable inhibitor of GPR84, a receptor implicated in various inflammatory pathways. This compound is useful for investigating GPR84-related diseases, particularly those driven by inflammation, such as inflammatory pain conditions. Its selective antagonism facilitates research in understanding the role of GPR84 in disease mechanisms and therapeutic potential. -
GPR84 Agonist
PSB-17365 is a potent agonist of the GPR84 receptor, demonstrating EC50 values of 2.5 nM in cAMP accumulation assays and 100 nM in β-arrestin 2 recruitment assays. This compound effectively stimulates GPR84 activity, making it a valuable tool for investigating the role of this receptor in inflammatory responses and immune modulation. Research applications include studies in metabolic disorders and the examination of GPR84's involvement in various physiological processes. -
GPR84 Antagonist
GPR84 Antagonist 3 is a selective antagonist of the G-protein-coupled receptor 84 (GPR84). This compound effectively inhibits GTPγS binding with a pIC50 value of 8.28, demonstrating its potency in modulating GPR84 activity. GPR84 Antagonist 3 is suited for research applications focused on exploring the role of GPR84 in inflammatory processes and metabolic regulation. Its favorable pharmacokinetic profile enhances its utility in pharmacological studies. -
GPR84 Agonist
ZQ-16 is a potent and selective agonist for the GPR84 receptor, exhibiting an EC50 value of 0.213 μM. This compound demonstrates specificity by showing no activity on other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119, and GPR120. ZQ-16 is useful in studies related to inflammation and immune responses, providing valuable insights into GPR84-mediated signaling pathways. -
GPR84 Agonist
OX04528 is a potent agonist of the GPR84 receptor, exhibiting G-protein biased activity. This compound demonstrates a remarkable ability to inhibit cAMP production, with an EC50 value of 0.00598 nM, and shows no signs of cytotoxicity. It is suitable for research applications focused on studying GPR84-related biological pathways and therapeutic targets. -
GPR84 Agonist
TUG-2208 is a potent agonist of GPR84, exhibiting a pEC50 of 8.98. This compound is characterized by its low lipophilicity, good solubility, and favorable in vitro permeability and microsomal stability. TUG-2208 is suitable for research applications investigating the role of GPR84 in various biological processes and potential therapeutic targets. -
GPR84 Antagonist
GPR84 antagonist 2 is a selective oral antagonist of the GPR84 receptor, exhibiting an IC50 of 8.95 nM. It demonstrates enhanced potency in calcium mobilization assays and effectively inhibits the chemotaxis of neutrophils and macrophages activated by GPR84. This compound is valuable for research into conditions such as ulcerative colitis, providing insights into immune regulation and inflammation. -
GPR84 Agonist
DL-175 is a selective GPR84 agonist known for its biased agonistic activity. This compound selectively activates functional responses in immune cells, promoting enhanced chemotaxis and phagocytosis in human bone marrow cells. As a potential chemical probe, DL-175 is valuable for research focused on immune response modulation and associated pathways. -
GPR84 Antagonist
GPR84 Antagonist 1 is a potent and selective competitive antagonist of human GPR84. It demonstrates high affinity for the receptor, making it an essential tool for investigating the role of GPR84 in inflammatory processes and immune responses. This compound is valuable in research applications focused on understanding GPR84-mediated signaling pathways and potential therapeutic interventions in related diseases. -
GPR84 Antagonist
GPR84 antagonist 9 is a selective antagonist of the G protein-coupled receptor GPR84, demonstrating an IC50 value of 0.012 μM. This compound is primarily utilized in research focusing on inflammatory-driven pain diseases, facilitating the investigation of its role in pain modulation and potential therapeutic applications. Its oral bioactivity supports in vivo studies aimed at understanding GPR84's contribution to inflammatory processes. -
GPR84 Agonist
GPR84 agonist-1 is a selective agonist of the GPR84 receptor, exhibiting an EC50 value of 2.479 μM. This compound is crucial for studying the physiological and pathological roles of GPR84 in immune responses, particularly in the context of septicemia. Researchers may utilize GPR84 agonist-1 to explore its potential therapeutic applications in inflammatory diseases and immune modulation. -
GPR84 Agonist
PSB-16434 is a selective agonist of G protein-coupled receptor 84 (GPR84). This compound demonstrates potential in the study of inflammatory diseases, metabolic disorders, and immune regulation by activating GPR84 signaling pathways. Its role in modulating immune responses makes it a valuable tool for researchers investigating novel therapeutic approaches in these areas. -
GPR88 Inhibitor
GPR88-IN-1 is a selective inhibitor of GPR88, a G protein-coupled receptor involved in modulating dopaminergic signaling. This compound demonstrates potential for investigating the role of GPR88 in various central nervous system disorders, including schizophrenia and drug addiction. It serves as a valuable tool for researchers exploring therapeutic pathways related to neuropsychiatric conditions. -
GPR88 Agonist
GPR88 agonist 2 is a potent agonist for the GPR88 receptor, exhibiting an EC50 of 14 µM in cAMP functional assays. This compound is notable for its ability to penetrate the blood-brain barrier, making it a valuable tool for neurological research. Its specific action on GPR88 provides insights into its role in neuropharmacology and related biological pathways. This compound is suitable for studies investigating the modulation of GPR88 in various physiological and pathological contexts. -
GPR88 Agonist
RTI-122 is a potent agonist of the GPR88 receptor, demonstrating effective brain penetration and a half-life of 5.8 hours in murine models. This compound exhibits a cAMP EC50 value of 11 nM, making it a valuable tool for investigating mechanisms associated with excessive drinking behaviors. Its metabolic stability and selective activity position RTI-122 as a significant reagent for research in addiction neuroscience and related fields. -
GPR88 Agonist
GPR88 Agonist 3 is a selective agonist of the G protein-coupled receptor GPR88, exhibiting an EC50 value of 204 nM. This compound is valuable for research into psychiatric and neurodegenerative disorders, providing insights into the modulation of signaling pathways involved in these conditions. Its GPR88 activation can contribute to understanding GPR88's role in brain function and potential therapeutic interventions. -
GPR81 Agonist
3-Chloro-5-hydroxybenzoic acid is a selective agonist of the lactate receptor GPR81, with an EC50 of 16 μM for human GPR81. This compound demonstrates significant biological activity, promoting lipolysis in a murine obesity model. It serves as a valuable tool for research focused on metabolic regulation and obesity-related pathways. -
GPR81 Agonist
GPR81 agonist 1 is a selective agonist targeting the GPR81 receptor, demonstrating EC50 values of 58 nM for human GPR81 and 50 nM for mouse GPR81. This compound effectively inhibits lipolysis in differentiated 3T3-L1 adipocytes and demonstrates an ability to suppress lipolysis in vivo in mouse models without causing cutaneous flushing. GPR81 agonist 1 exhibits significant selectivity for GPR81 over GPR109a, making it a valuable tool for research into metabolic regulation and adipocyte biology.
