Catalog No.
Product Name
Application
Product Information
Citations
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MrgprX2 Antagonist
MrgprX2 antagonist-9 is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MrgprX2) with an IC50 value ranging from 0.1 to 100 nM. This compound exhibits significant potential for investigating the role of MrgprX2 in inflammatory processes. Its application in research can enhance the understanding of pain signaling and other pathophysiological conditions linked to this receptor. -
MrgprX1 Positive Allosteric Modulator
BCFTP is a potent and selective positive allosteric modulator of the human Mas-related G protein-coupled receptor X1 (MrgprX1). It enhances MrgprX1 signaling in HEK293 cells and effectively alleviates neuropathic pain-related behaviors in a humanized mouse model of chronic constrictive injury, demonstrating a MrgprX1-dependent mechanism. BCFTP has the potential to synergistically enhance the analgesic effects of psychoactive substances in this model. This compound serves as a valuable tool for research into neuropathic pain mechanisms and potential therapeutics. -
MrgprX2 Antagonist
MrgprX2 antagonist-3 is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MrgprX2), primarily involved in mediating pruritic and inflammatory signaling. This compound exhibits significant efficacy in inhibiting MrgprX2-related pathways, making it a valuable tool for studying inflammatory skin disorders. Research applications include investigations into the role of MrgprX2 in various dermatological conditions and the development of novel therapeutic strategies targeting these pathways. -
MRGPRX2 Agonist
(R)-ZINC-3573 is a selective agonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2), exhibiting an EC50 value of 740 nM. This compound serves as an effective probe for studying the biological functions of MRGPRX2, particularly in relation to pain and itch mechanisms. Its application in research contributes to understanding receptor signaling pathways and exploring therapeutic targets for related conditions. -
MRGPRX2 Antagonist
ZINC49534341 is an antagonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2) with a binding affinity (Ki) of 32 nM. This compound negatively regulates MRGPRX2-mediated signaling pathways, demonstrating utility in research related to pain, inflammation, and mast cell activation. It serves as a valuable tool for investigating the role of MRGPRX2 in various biological processes and for potential therapeutic applications. -
MRGPR X4 Modulator
Nelremagpran is a potent modulator of MRGPR X4, exhibiting antagonist activity with an IC50 of less than 100 nM. This compound is valuable for investigating autoimmune diseases, including psoriasis, multiple sclerosis, Stevens-Johnson syndrome, and various chronic itch conditions. Its ability to selectively inhibit MRGPR X4 makes it a crucial tool for elucidating the role of this receptor in disease pathology and for the development of targeted therapeutic strategies. -
MrgprX2 Antagonist
MrgprX2 antagonist-5 is a selective antagonist of the MrgprX2 receptor, involved in the modulation of inflammatory responses. This compound demonstrates significant potential for the investigation of skin inflammatory disorders, particularly in elucidating the role of MrgprX2 in pathophysiological processes. Its application in research may enhance the understanding of therapeutic strategies targeting the MrgprX2 pathway. -
MRGPR X4 Modulator
MRGPRX4 modulator-1 is a potent antagonist of the mas-related G-protein receptor X4 (MRGPR X4), exhibiting an IC50 of less than 100 nM. This compound is valuable for investigating MRGPR X4-dependent pathologies, including itch, pain, and autoimmune disorders. Its ability to modulate MRGPR X4 activity makes it a crucial tool for research into these challenging conditions. -
MRGPRX1 Agonist
MRGPRX1 agonist 1 is a potent agonist of the Mas-related G protein-coupled receptor X1 (MRGPRX1), demonstrating an EC50 of 50 nM and over 50-fold selectivity against δ, μ, and κ opioid receptors. This compound is ineffective against MRGPRC11, which plays a role in inhibiting high voltage-activated (HVA) Ca2+ currents, thereby reducing neurotransmitter release and influencing nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is valuable for investigating mechanisms of chronic pain, particularly neuropathic pain, facilitating research into potential therapeutic strategies. -
MRGPRX2 Modulator
MRGPRX2 modulator-1 is a selective modulator of the mas-related G-protein coupled receptor X2 (MRGPRX2). It exhibits significant biological activity in modulating nociceptive pathways, making it a valuable tool for investigating mechanisms associated with inflammation, pain perception, and autoimmune disorders. This compound facilitates research into therapeutic strategies targeting MRGPRX2 in order to develop novel approaches for managing pain and inflammatory conditions. -
MrgprX2 Antagonist
MrgprX2 antagonist-4 is an antagonist of the Mas-related G protein-coupled receptor X2 (MrgprX2). This compound demonstrates significant biological activity in modulating inflammatory responses, making it valuable for research into skin inflammatory disorders. Its application can aid in understanding the pathways involved in skin inflammation and contribute to the development of therapeutic strategies targeting this receptor. -
MRGPRX4 Agonist
PSB-22034 is a selective agonist of the MRGPRX4 receptor, demonstrating EC50 values of 11.2 nM in Ca2+ mobilization assays and 30.0 nM in β-arrestin recruitment assays. This compound is valuable for investigating the physiological roles of MRGPRX4 and its involvement in pain, neurogenic inflammation, and other pathological processes. Its precise modulation of MRGPRX4 provides a tool for elucidating receptor functions in various biological contexts. -
MRGPRX4 Antagonist
1-(4-Fluorobenzyl)-1H-indazole-3-carboxylic acid acts as an antagonist of the Mas-related G protein-coupled receptor X4 (MRGPRX4). This compound, a metabolite of AB-FUBINACA, exhibits significant biological activity relevant to the modulation of pain and inflammation pathways. It is a valuable research tool for studying GPCR-related mechanisms and developing new therapeutic strategies targeting MRGPRX4. -
MRGPRX2 Modulator
MRGPRX2 modulator-3 is a selective modulator targeting the Mas-related G protein-coupled receptor X2 (MRGPRX2). This quinoline derivative exhibits significant potential in the modulation of various biological responses linked to MRGPRX2 activation. It is applicable in studies investigating MRGPRX2-related pathologies, including allergies, pruritus, pain, inflammation, and autoimmune disorders, making it a valuable tool for advancing research in these areas. -
MRGPRX1 PAM
MRGPRX1 agonist 4 is a potent positive allosteric modulator of the Mas-related G protein-coupled receptor X1 (MRGPRX1), exhibiting an EC50 value of 0.1 μM. This compound demonstrates favorable metabolic stability and oral bioavailability. MRGPRX1 agonist 4 has been shown to alleviate behavioral heat hypersensitivity in humanized MRGPRX1 mice models of neuropathic pain, making it a valuable tool for research in pain modulation and related therapeutic applications. -
MRGPRC11 Agonist
JHU-58 is a peptidomimetic agonist specifically targeting the MRGPRC11 receptors in mice and rats. It exhibits notable analgesic properties in mouse models of neuropathic pain, highlighting its potential for therapeutic applications. This reagent serves as a valuable tool for investigating the mechanisms underlying neuropathic pain and exploring novel pain management strategies. -
MRGPRX1 PAM
MRGPRX1 Agonist 2 is a potent positive allosteric modulator of the Mas-related G protein-coupled receptor X1 (MRGPRX1) with an EC50 value of 0.48 μM. This compound is primarily utilized in research focused on neuropathic pain, enabling the exploration of MRGPRX1's role in pain pathways. Its distinct mechanism of action makes it a valuable tool for understanding the modulation of nociceptive signals. -
MRGPRX2 Antagonist
MrgprX2-IN-1 is a selective antagonist of the Mas-related G-protein coupled receptor X2 (MRGPRX2). This compound effectively inhibits IgE-independent immune responses by blocking MRGPRX2-mediated mast cell degranulation and the subsequent release of inflammatory mediators. MrgprX2-IN-1 serves as a valuable tool for investigating pseudo-allergic reactions, chronic pruritus, and various inflammatory diseases. -
MRGPRD Agonist
(Rac)-EP-2825 is a MRGPRD agonist exhibiting an IC50 value between 100 and 500 nM. It plays a significant role in pain research, providing insights into the mechanisms of nociception and potential therapeutic interventions. This compound facilitates the exploration of MRGPRD pathways, contributing to a better understanding of pain modulation and associated biological processes. -
MRGPRX2 Antagonist
MrgprX2-IN-2 is a selective antagonist of the Mas-related G-protein coupled receptor X2 (MRGPRX2). By inhibiting MRGPRX2-mediated mast cell degranulation, MrgprX2-IN-2 effectively blocks IgE-independent immune responses, thereby reducing the release of inflammatory mediators. This compound is valuable for studies investigating pseudo-allergic reactions, chronic pruritus, and various inflammatory diseases. -
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. -
RZR/ROR Receptor Agonists
CGP52608 is a selective agonist for the RZR/ROR receptor, exhibiting notable anti-tumor activity with minimal interaction with the cell surface G-protein coupled melatonin receptor. This compound has been demonstrated to inhibit the proliferation of mouse 16/C breast cancer cells, making it a valuable tool in cancer research. Additionally, CGP52608 is effective in inducing vesicle formation in diatoms, providing insights into cellular mechanisms and developmental 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.
