Catalog No.
Product Name
Application
Product Information
Citations
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Gpr120 agonist
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of ?7.62. -
EBI2 inverse agonist
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM. -
GPR40 agonist
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. -
FFAR1/GPR40 activator
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. -
GPR40 activator
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1. -
GPR88 receptor agonist
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay. -
GPR40 agonist
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. -
cell permeable TgPrxII inhibitor
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII). -
GPR109A agonist
Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease. -
GPR35 agonist
Pamoic acid disodium is a potent agonist of GPR35, with an EC50 of 79 nM. It induces GPR35 internalization and activates ERK1/2 signaling with EC50 values of 22 nM and 65 nM, respectively. Additionally, it effectively recruits β-arrestin2 to GPR35 and exhibits antinociceptive properties, supporting its potential in pain research. -
GPR55 antagonist
ML192 is a selective antagonist of G protein-coupled receptor 55 (GPR55), effectively inhibiting GPR55-mediated signaling pathways. It blocks β-arrestin trafficking, suppresses ERK1/2 phosphorylation, and prevents PKCβII translocation, thereby interfering with downstream cellular responses. ML192 is a valuable tool for studying the physiological and pathological roles of GPR55 in processes such as inflammation, pain, cancer, and metabolic regulation. -
GPR35 agonist
Pamoic acid (Embonic acid) is a potent agonist of G protein-coupled receptor 35 (GPR35), with an EC₅₀ of 79 nM. Activation of GPR35 by pamoic acid is associated with both neuroprotective and anti-inflammatory effects, making it a valuable compound for research into neurological disorders and inflammatory diseases. Its pharmacological profile suggests potential therapeutic applications in conditions where GPR35-mediated signaling plays a regulatory role. -
GPR18 Agonist
N-Arachidonylglycine (NA-Gly) selectively acts as an agonist for the GPR18 receptor, exhibiting an EC50 value of 44.5 nM. Unlike its structural analog anandamide, NA-Gly does not engage with CB1 or CB2 receptors. This compound also demonstrates inhibitory activity on GLYT2 with an IC50 of 5.1 μM. Additionally, N-Arachidonylglycine has been shown to effectively promote the migration of endometrial cells, making it a valuable tool for research in cellular migration and cannabinoid receptor activity. -
MRGPRX2 Antagonist
GE1111 is an antagonist of the MRGPRX2 receptor, with an IC50 value of 9.4 μM. This compound effectively inhibits MRGPRX2/MRGPRB2-mediated mast cell activation, leading to the reduction of pro-inflammatory cytokines, including TSLP, IL-13, MCP-1, TNF-α, and IL-1β. Additionally, GE1111 preserves claudin 1 and involucrin expression, enhances macrophage phagocytic activity, and modulates STIM1 and phosphorylated AKT activation. Its anti-inflammatory and anti-allergic properties make GE1111 relevant for research in conditions such as rosacea, atopic dermatitis, and ulcerative colitis. -
GPRC5D/CD3ε/TNFRSF17 Antibody
Ramantamig is a humanized monoclonal antibody that targets CD3ε on T cells, as well as GPRC5D and TNFRSF17 (BCMA) on multiple myeloma cells. It facilitates T-cell-mediated cytotoxicity by forming immunological synapses, leading to selective killing of myeloma cells without non-specific T-cell activation when target cells are absent. Additionally, Ramantamig has been engineered to minimize interactions with Fc receptors, enhancing its specificity. This reagent is ideal for research in multiple myeloma therapies. -
GPR68 Inhibitor
Ogremorphin is a selective inhibitor of the G protein-coupled receptor GPR68. This compound exhibits notable anti-inflammatory and anti-tumor properties, demonstrating the ability to inhibit the migration of human melanoma cells and induce ferroptosis in glioblastoma cells. Ogremorphin is a valuable tool for researchers investigating the roles of GPR68 in cancer biology and inflammation. -
Anticancer Agent/Immune Modulator/GPR120 Activator
Phytosphingosine is a bioactive sphingolipid that functions primarily as an immunomodulator and activator of GPR120. Exhibiting anti-inflammatory, antibacterial, and anticancer properties, Phytosphingosine can induce apoptosis in various cell types. Its role in regulating immune responses makes it a valuable reagent for research on inflammatory skin diseases and type II diabetes. Additionally, with an IC50 value of 33.4 μM, Phytosphingosine enhances understanding of GPR120-mediated pathways. -
GPR35 Agonist
Bufrolin is a potent agonist of GPR35, known for its ability to promote the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. This compound exhibits significant antiallergic properties by stabilizing mast cells and inhibiting inflammatory responses associated with internalization peptides. Bufrolin is valuable for research into anti-inflammatory mechanisms and therapeutic applications targeting GPR35-related pathways. -
GPR91 Ligand
Succinate calcium primarily targets the G protein-coupled receptor GPR91 and serves as a significant intermediate in the citric acid cycle. This compound is known to enhance the amplitude of calcium transients in cardiac muscle cells while also accelerating their decay rate. Additionally, succinate calcium has been implicated in inducing myocardial apoptosis, making it valuable for research into cardiac physiology and pathology. -
GPR75 Inhibitor
(Rac)-AAA is a potent inhibitor of GPR75, targeting the receptor to modulate key signaling pathways. This compound effectively blocks the downregulation of GPR75 expression induced by 20-HETE, leading to the inhibition of downstream pathways such as EGFR, AKT, NF-κB, and FAK. (Rac)-AAA also reverses 20-HETE-mediated epithelial-mesenchymal transition, characterized by the downregulation of vimentin and upregulation of E-Cadherin, while reducing MMP-2 activity and cancer cell migration. Additionally, it mitigates the upregulation of HIC-5 and affects the localization of PKC-α and phosphorylated AKT, making (Rac)-AAA a significant tool in the study of castration-resistant prostate cancer. -
GPR35 Activator
DHICA is a GPR35 agonist that acts as both an eumelanin building block and a melanin synthesis intermediate. It activates GPR35, leading to dynamic mass redistribution and β-arrestin translocation. Additionally, DHICA promotes single-strand breaks in plasmid DNA and enhances the activity and expression levels of superoxide dismutase (SOD) and catalase. This compound is relevant for research applications in skin cancer and colon cancer studies. -
HGPRT Inhibitor
8-Azahypoxanthine is a purine analog that functions as an inhibitor of hypoxanthine-guanine phosphoribosyltransferase (HGPRT). This compound demonstrates antitumor activity, making it a valuable tool in cancer research, particularly for studying adenocarcinoma and other tumor types. Its ability to inhibit HGPRT may provide insights into the mechanisms of tumor growth and potential therapeutic strategies. -
GPR17 Antagonist
RWT9996 is a selective antagonist of GPR17, functioning by inhibiting G protein activation and β-arrestin-2 recruitment prompted by MDL-29951. This compound effectively reduces ERK/CREB phosphorylation and the accumulation of inositol phosphates in response to MDL-29951 stimulation. RWT9996 is valuable for research into neurological disorders, providing insights into the role of GPR17 in various pathophysiological processes. -
GPR55 Agonist
20:4 Lyso PI is a selective agonist of the G protein-coupled receptor GPR55, exhibiting a potency with an EC50 value of 10 nM in inducing cell rounding in GPR55-expressing HEK293 cells. This compound activates RhoA, leading to ROCK-dependent cytoskeletal rearrangement, and stimulates the ERK signaling pathway while increasing intracellular free calcium levels. 20:4 Lyso PI is valuable for research into immune diseases and related cellular signaling mechanisms. -
GPR119 Agonist
2-Oleoylglycerol is a GPR119 agonist that activates hGPR119 in transiently transfected COS-7 cells with an EC50 value of 2.5 μM. This lipid enhances the inflammatory response in macrophages and promotes fibrosis through the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. Additionally, 2-Oleoylglycerol stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. Its effects make it a valuable tool for research into non-alcoholic steatohepatitis (NASH) and related metabolic disorders. -
GPR34 Receptor Antagonist
GPR34 Receptor Antagonist 2 is an antagonist that specifically targets the GPR34 receptor. This compound exhibits significant activity in modulating immune responses, making it a valuable tool for investigating inflammatory diseases and other immune-related disorders. Its potential applications in research include studying the pathophysiology of immune diseases and developing novel therapeutic strategies. -
GPR34 Receptor Antagonist
GPR34 receptor antagonist 3 is a selective antagonist of the GPR34 receptor, with an IC50 value of 0.680 μM. This compound effectively inhibits ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent manner, demonstrating minimal cytotoxicity. GPR34 receptor antagonist 3 is valuable for research into the modulation of sensory signaling pathways and has shown antisensory activity in mouse models of neuropathic pain. -
hGPR132a Antagonist
GSK1820795A is a selective antagonist of the human GPR132a receptor, effectively inhibiting its activation by N-acylamides in yeast cell models. This compound also functions as an antagonist of angiotensin II and has partial agonist activity at PPARγ. It serves as a valuable tool for research into metabolic disorders and receptor signaling pathways. -
FFA1/GPR40 Agonist
HWL-088 is a potent agonist of free fatty acid receptor 1 (FFA1/GPR40) with an EC50 of 18.9 nM, exhibiting moderate activity on PPARδ with an EC50 of 570.9 nM. This compound enhances glucose and lipid metabolism, demonstrating significant anti-diabetic effects. HWL-088 is valuable for research investigating metabolic disorders and insulin sensitivity. -
GPR84 Antagonist
TUG-2181 is a GPR84 antagonist, exhibiting an IC50 value of 34 nM. This compound effectively inhibits reactive oxygen species (ROS) production and interleukin-8 (IL-8) release in human neutrophils stimulated by GPR84 agonists. TUG-2181 is particularly valuable for research exploring the mechanisms of inflammation and fibrosis. -
GPR84 Agonist/AKR1C3 Inhibitor
Pyrone-211 is a potent agonist of the GPR84 receptor and an inhibitor of AKR1C3. This compound plays a significant role in modulating the expanded polyamine pathway, making it valuable for research in inflammation and metabolic diseases. Its dual functionality as both a receptor agonist and enzyme inhibitor positions Pyrone-211 as a useful tool for exploring cellular signaling and therapeutic interventions in related pathways. -
DPP-4/GPR119 Modulator
DPP-4/GPR119 Modulator 1 is a dual-functional compound that serves as an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and a GPR119 agonist. This compound exhibits significant blood glucose-lowering effects and demonstrates moderate hERG channel inhibition with an IC50 of 4.9 μM. DPP-4/GPR119 Modulator 1 is particularly valuable in diabetes research and functions as a click chemistry reagent, possessing an alkyne group that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules. -
DPP-4/GPR119 Modulator
DPP-4/GPR119 modulator 2 is a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist, exhibiting an IC50 of 0.22 μM for DPP-IV and an EC50 of 0.95 μM for GPR119. This compound is pertinent for diabetes research, facilitating studies on metabolic regulation and insulin secretion. Additionally, it features an alkyne group, enabling its use in click chemistry applications through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
HGPRT/TBrHGPRT1 Inhibitor
HGPRT/TBrHGPRT1-IN-1 is a selective inhibitor of human hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and Trypanosoma brucei HGPRT1 (TBrHGPRT1), with a Ki value of 3 nM for both targets. This compound effectively reduces cell growth through its targeted inhibition mechanism. HGPRT/TBrHGPRT1-IN-1 is particularly valuable for research applications in the fields of infectious diseases and oncology. -
HGPRT Inhibitor
2′-Deoxy-GDP trisodium is a potent inhibitor of hypoxanthine phosphoribosyltransferase (HGPRT), exhibiting an IC50 value of 12.5 μM. As a guanosine monophosphate (GMP) analogue, it plays a significant role in research related to purine metabolism and the recycling pathway in protozoan parasites. This reagent is valuable for studying HGPRT's function and its implications in parasitic diseases. -
GPR39 Agonist
Glycolithocholic acid 3-sulfate disodium functions as a GPR39 agonist, exhibiting EC50 values of 47.9 and 66.8 μM in the absence of Zn2+, and 8 and 8.7 μM in the presence of Zn2+ in M39-20 and hGPR39-2 cell lines, respectively. This compound activates GPR39 receptors to promote intracellular calcium signaling without relying on Zn2+ binding sites H17 and H19. Additionally, it demonstrates the ability to inhibit HIV-1 replication in vitro. Glycolithocholic acid 3-sulfate disodium is a valuable tool for investigating HIV infection and gallbladder disease mechanisms. -
GPR15 Antagonist
GPR15 antagonist-1 is a selective antagonist of the G protein-coupled receptor 15 (GPR15). This compound is implicated in critical biological processes related to HIV infection, colonic inflammation, and smoking-related diseases. GPR15 antagonist-1 serves as a valuable tool for research exploring the therapeutic potential of modulating GPR15 activity in various pathological contexts. -
GPR120 Agonist
9-PAHSA is a potent endogenous agonist of the GPR120 receptor, demonstrating an EC50 of 18 μM. This compound effectively inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, 9-PAHSA promotes adipocyte browning, enhances glucose uptake, and diminishes lipid accumulation, while supporting mitochondrial function in steatotic hepatocytes. It also exhibits neuroprotective effects by modulating the expression of REST and BDNF in the prefrontal cortex of diabetic mice, preventing cognitive deficits and abnormal social behaviors. 9-PAHSA is valuable for research into diabetes-related cognitive impairment, obesity, and non-alcoholic fatty liver disease. -
GPRC5A Agonist
7-Fluorotryptamine hydrochloride acts as a potent agonist of GPRC5A, promoting β-arrestin recruitment through GPRC5A activation. This compound is valuable for studying immune and cancer signaling pathways, providing insights into the mechanisms of GPRC5A in various biological contexts. Its role in modulating receptor activity makes it a useful tool for researchers investigating related biochemical processes.
