Catalog No.
Product Name
Application
Product Information
Citations
-
GPR35 Agonist
GPR35 Agonist 2 is a highly effective compound that specifically activates the GPR35 receptor, demonstrating EC50 values of 26 nM and 3.2 nM in β-arrestin recruitment and Ca2+ release assays, respectively. This agonist plays a significant role in advancing research related to GPR35 signaling pathways and their implications in various physiological processes. Its potent activity makes it suitable for studies investigating the therapeutic potential of targeting GPR35 in metabolic and inflammatory conditions. -
GPR183 Inverse Agonist
GPR183 inverse agonist-1 is a potent inverse agonist targeting the G protein-coupled receptor GPR183. It effectively inhibits GPR183-mediated Gi activation and prevents β-arrestin2 recruitment, thereby blocking the migration of peripheral blood mononuclear cells (PBMCs). This compound is valuable for research into inflammatory, autoimmune, and neoplastic disorders, enabling scientists to explore its therapeutic potential in these fields. -
GPR18 Agonist
PSB-KK1415 is a selective agonist for the human orphan G protein-coupled receptor GPR18, exhibiting an EC50 value of 19.1 nM. This compound has been identified to modulate receptor activity and can be utilized in various biological research applications, including studies of neurological processes and potential therapeutic pathways. Its specificity for GPR18 makes it a valuable tool for exploring receptor signaling mechanisms and their implications in health and disease. -
GPR18 Agonist
PSB-KK1445 is a potent and selective GPR18 agonist, exhibiting EC50 values of 45.4 nM for human GPR18 and 124 nM for mouse GPR18. It demonstrates over 200-fold selectivity against both cannabinoid receptor subtypes, GPR55, and GPR183. This compound is valuable for research applications exploring the physiological roles of GPR18 in various biological processes and potential therapeutic uses related to the endocannabinoid system. -
GPR55 Antagonist
PSB-SB-487 is a potent antagonist of GPR55, exhibiting an IC50 value of 0.113 µM, and acts as an agonist for the CB2 receptor with a Ki value of 0.292 µM. This compound is valuable for investigating various biological processes and disease states, including diabetes, Parkinson’s disease, neuropathic pain, and cancer. Its dual activity makes it a significant tool for understanding the role of cannabinoid receptors in disease mechanisms and potential therapeutic interventions. -
GPR55 Fluorescent Ligand
Tocrifluor 1117 is a selective fluorescent ligand targeting the GPR55 receptor. This compound serves as a valuable tool in research for visualizing the cellular distribution of cannabinoid receptors, including GPR55, in live tissues. With excitation and emission maxima at 543 nm and 590 nm, respectively, Tocrifluor 1117 enhances the understanding of cannabinoid receptor localization and function in various biological contexts. -
GPR18 Agonist
PSB-KD107 is an agonist of the GPR18 receptor, a cannabinoid-activated orphan G-protein-coupled receptor. This compound exhibits anti-inflammatory activity and is applicable in research related to Duchenne muscular dystrophy, making it a valuable tool for investigating inflammation-related pathways and therapeutic interventions in muscle degeneration. -
GPR133 Agonist
AP-503 is a selective agonist of GPR133 (also known as ADGRD1), exhibiting an EC50 value of 1.21 nM. This compound is of significant interest in research focused on mitigating muscle-related diseases and addressing vestibular dysfunction. Its precise modulation of GPR133 activity presents opportunities for elucidating the receptor's role in associated physiological pathways. -
GPR17 Modulator
ASN02563583 is a GPR17 modulator that exhibits an IC50 value of 0.64 nM in the [35S]GTPγS binding assay, indicating its potency in regulating GPR17 receptor activity. This compound is particularly relevant for research focused on neurological diseases, providing insights into the role of GPR17 in related pathophysiological processes. -
GPR17 Antagonist
GPR17 Antagonist 1 is a selective antagonist of the GPR17 receptor, which is involved in various physiological processes. This compound exhibits significant inhibitory activity on GPR17, making it a valuable tool for studying metabolic disorders such as diabetes and obesity. Its application in pharmacological research contributes to the understanding of GPR17's role in these diseases and may aid in the development of therapeutic strategies. -
GPR17 Agonist
ASN04421891 is a potent GPR17 agonist, exhibiting nanomolar EC50 and high specificity. This compound facilitates the maturation of oligodendrocyte precursor cells into mature myelinating oligodendrocytes, making it a valuable tool for investigating neurodegenerative diseases. ASN04421891 is applicable in research related to cerebral and cardiac ischemia, multiple sclerosis, schizophrenia, depression, Alzheimer's disease, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis (ALS), and various neuroinflammatory disorders. -
GPR110 Agonist
GPR110 peptide agonist P12 is an agonist targeting the GPR110 receptor. This peptide significantly enhances the initial rate of G protein GTPγS binding stimulated by GPR110, effectively mimicking natural ligands. By inducing dissociation between the receptor's extracellular domain and its seven transmembrane domains, P12 exposes the β-strand-13/stalk region of the 7TM domain, facilitating G protein signaling activation. This compound is valuable for research into developmental disorders and cancers associated with GPR110 pathways. -
GPR17 Modulator
GPR17 modulator-1 is a potent modulator of the G protein-coupled receptor GPR17, exhibiting an IC50 of less than 10 nM for human GPR17 in CHO cells. This compound demonstrates moderate pharmacokinetic properties in murine models and is capable of crossing the blood-brain barrier. GPR17 modulator-1 is valuable for research focused on neuroinflammatory disorders and central nervous system-related applications. -
SUCNR1 (GPR91) Antagonist
NF-56-EJ40 is a highly selective antagonist of the human SUCNR1 (GPR91), demonstrating potent inhibitory activity with an IC50 of 25 nM and a Ki of 33 nM. Its specificity minimizes interaction with rat SUCNR1, showcasing a Ki value of 17.4 nM when assessed against a humanized rat model. This compound is valuable for research applications targeting metabolic disorders and the role of SUCNR1 in physiological processes. -
hGPR91 Antagonist
hGPR91 antagonist 3 is a selective antagonist of the human GPR91 receptor, exhibiting potent inhibition with IC50 values of 35 nM and 135 nM for human and rat GPR91, respectively. This compound serves as a valuable tool in research applications focused on metabolic regulation, inflammation, and immune response modulation. Its oral bioactivity further enhances its utility in in vivo studies related to GPR91-mediated signaling pathways. -
SUCNR1 (GPR91) Antagonist
NF-56-EJ40 hydrochloride is a selective antagonist of the human SUCNR1 (GPR91) receptor, exhibiting an IC50 of 25 nM and a Ki of 33 nM. This compound demonstrates minimal activity against rat SUCNR1 while maintaining high affinity for humanized rat SUCNR1, evidenced by a Ki value of 17.4 nM. NF-56-EJ40 hydrochloride is suitable for research applications investigating the role of SUCNR1 in metabolic and cardiovascular diseases. -
GPR109B Agonist
D-Kynurenine functions as an agonist for the G protein-coupled receptor GPR109B. This compound acts as a bioprecursor for kynurenic acid (KYNA) and 3-hydroxykynurenine, making it relevant for studies involving metabolic pathways. Additionally, D-kynurenine is utilized in fluorometric assays for D-amino acid oxidase and has been shown to promote epithelial-to-mesenchymal transition through the activation of the aryl hydrocarbon receptor (AHR), highlighting its potential applications in cancer research and cellular biology. -
ASGPR Ligand
tri(GalNAc-PEG2)-PEG4-cyclo(Ac-DCAW-{Arg(3F-Ph)-PEG2}-LGELVWCT) (Cys2-Cys12) is a potent ligand for the asialoglycoprotein receptor (ASGPR), facilitating targeted delivery to lysosomes. This compound is specifically designed for applications in lysosome-targeting chimera (LYTAC) research, offering enhanced cellular uptake and improved therapeutic efficacy. Its unique structure enables effective receptor recognition and binding, making it a valuable tool for studying ASGPR-mediated pathways. -
GPR34 Antagonist
YL-365 is a potent and selective antagonist of the GPR34 receptor, exhibiting an IC50 value of 17 nM. By binding to a specific region within the orthosteric binding pocket, YL-365 induces allosteric modifications that stabilize the receptor in an inactive state. It effectively down-regulates the pro-inflammatory gene iNOS in M1 microglia, consequently suppressing pro-inflammatory responses. Additionally, YL-365 demonstrates dose-dependent reduction of mechanical allodynia in mouse models of neuropathic pain, making it a valuable tool for studying inflammatory mechanisms and potential treatments for neuropathic conditions. -
GPR3 Agonist
GPR3 Agonist-2 is a potent full agonist of the G protein-coupled receptor 3 (GPR3), exhibiting an IC50 of 260 nM. This compound is instrumental in studies exploring the physiological and pathological roles of GPR3, including its involvement in neurodevelopment and potential implications in neurodegenerative diseases. GPR3 Agonist-2 serves as a valuable tool for research applications in signaling pathways mediated by GPR3. -
GPR17 Agonist
GPR17 Agonist 1 is a selective and potent agonist of the GPR17 receptor with an EC50 value of 35 pM. This compound demonstrates weak activation of the P2Y receptor, making it a useful tool for studies related to neurobiology. GPR17 Agonist 1 is particularly applicable in research focused on neurological diseases, offering insights into receptor signaling and its implications in various pathophysiological conditions. -
GPR27 Agonist
PT-91 is a potent agonist of the GPR27 receptor, known for its ability to enhance receptor activation. This compound demonstrates significant metabolic stability and effective brain exposure in murine models, making it a valuable tool for investigating the role of GPR27 in neurological research and potential therapeutic applications. Its unique profile supports studies related to neurodegenerative diseases and cognitive functions. -
Anti-GPRC5D Antibody
Vemzatatug is a humanized IgG1κ monoclonal antibody that targets GPRC5D, playing a crucial role in antitumor activity. This reagent is particularly relevant for research involving multiple myeloma (MM) and may aid in understanding tumor progression and therapeutic responses. It serves as a valuable tool for exploring GPRC5D's role in cancer biology and therapeutic interventions. -
GPR17 Agonist
PSB-1737 is a selective agonist of the GPR17 receptor, exhibiting an EC50 of 270 nM for human GPR17, with significantly reduced activity on murine GPR17 (EC50 > 10 μM). This compound does not exhibit significant inhibition at the glycine binding site of NMDA receptors, nor does it show notable activity on P2Y receptor subtypes. PSB-1737 is valuable for research in the context of demyelinating diseases, such as multiple sclerosis, and inflammatory-related anemia. -
GPR34 Agonist
GPR34 Agonist 1 is a lysophosphatidylserine analogue that selectively activates the GPR34 receptor. This compound facilitates the modulation of GPR34-mediated signaling pathways, making it a valuable tool for investigating the physiological roles of this receptor in various biological processes. Its utility extends to research areas such as immunology and neurobiology, where GPR34 activity is implicated in inflammation and neurodevelopment. -
GPR18 Inhibitor
PSB-CB-27 is a potent and selective inhibitor of the GPR18 receptor with an IC50 of 0.65 μM. It exhibits a high degree of selectivity over human GPR55, CB1, and CB2 receptors. This compound effectively blocks GPR18 activation induced by Δ9-Tetrahydrocannabinol (THC), making it a valuable tool for investigating the roles of GPR18 in inflammatory diseases and cancer immunotherapy research. -
P2Y2R/GPR17 Antagonist
P2Y2R/GPR17 antagonist 1 is a selective antagonist targeting both the P2Y2 receptor (P2Y2R) and G protein-coupled receptor 17 (GPR17), with IC50 values of 3.17 µM and 1.67 µM, respectively. This compound exhibits promising metabolic stability in human liver microsomes, making it a valuable tool for research. It is particularly applicable in studies involving purinergic signaling and neuroinflammation, providing insights into therapeutic strategies for related diseases. -
MrgprX2 Antagonist
MrgprX2 antagonist-1 is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MrgprX2). It exhibits potent inhibition of MrgprX2-mediated signaling, making it valuable for investigating the role of this receptor in various inflammatory skin disorders. This compound is suitable for research applications aimed at understanding and potentially developing therapeutic interventions for inflammatory conditions involving MrgprX2. -
MrgprX2 Antagonist
MrgprX2 antagonist-8 is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MrgprX2). It effectively inhibits MrgprX2 signaling, making it useful for investigating the role of this receptor in various inflammatory disorders. This compound is valuable for research applications targeting pain perception, allergic responses, and other related conditions influenced by MrgprX2 modulation. -
MrgprX2 Antagonist
MrgprX2 antagonist-2 is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MrgprX2). This compound has demonstrated significant activity in modulating inflammatory responses, making it a valuable tool for investigating cutaneous inflammatory disorders. Its application may facilitate the understanding of MrgprX2 signaling pathways in skin-related research. -
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.
