Catalog No.
Product Name
Application
Product Information
Citations
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GPR119 Agonist
BMS-986034 is a selective agonist of the GPR119 receptor, which plays a significant role in glucose homeostasis and insulin secretion. This compound demonstrates notable efficacy in enhancing glucose-dependent insulin release and may contribute to the regulation of appetite and energy balance. BMS-986034 is primarily utilized in research related to metabolic disorders, including type 2 diabetes and obesity, making it a valuable tool for investigating therapeutic strategies targeting the GPR119 pathway. -
GPR119 Agonist
AS1907417 is a selective agonist of GPR119, demonstrating oral bioactivity. This compound exhibits antihyperglycemic properties, making it a valuable tool in the study of type 2 diabetes and related metabolic disorders. Its unique chemical structure enhances its potential for research applications targeting glucose homeostasis and insulin sensitivity. -
GPR119 Agonist
GSK1104252A is a potent and selective agonist of the GPR119 receptor. This compound demonstrates significant insulinotropic activity, making it relevant for research applications focused on type 2 diabetes and metabolic disorders. Its ability to enhance glucose-dependent insulin secretion positions GSK1104252A as a valuable tool for exploring therapeutic strategies in glycemic control. -
GPR-119 Agonist
MK-8282 is a potent, orally active agonist of the GPR-119 receptor. This compound has demonstrated the ability to improve glucose tolerance, making it a valuable tool for investigating metabolic disorders. MK-8282 is primarily utilized in research focused on type 2 diabetes and its associated pathways. -
GPR119 Agonist
PSN 375963 hydrochloride is a potent agonist of GPR119, exhibiting EC50 values of 8.4 μM and 7.9 μM for human and mouse GPR119, respectively. This compound demonstrates comparable efficacy to the endogenous agonist oleoylethanolamide (OEA). PSN 375963 hydrochloride is valuable for research applications targeting metabolic disorders and the modulation of glucose homeostasis. -
GPR119 Agonist
BMS-903452 is a selective agonist of GPR119, a G protein-coupled receptor implicated in glucose metabolism and insulin secretion. This compound enhances the release of incretin hormones, which play a crucial role in regulating blood sugar levels. BMS-903452 is primarily utilized in diabetes research to explore potential therapeutic avenues for the management of type 2 diabetes and related metabolic disorders. -
GPR119 Agonist
GSK2041706A is a potent agonist of the G protein-coupled receptor 119 (GPR119). This compound has demonstrated significant biological activity in modulating glucose metabolism and insulin secretion, making it a valuable tool in the research of type 2 diabetes. Its ability to activate GPR119 positions it as a promising candidate for studies focusing on metabolic disorders and potential therapeutic interventions. -
GPR119 Agonist
GSK-1292263 hydrochloride is a potent orally active agonist of GPR119, demonstrating a pEC50 of approximately 6.9 nM for human GPR119 and 6.7 nM for rat GPR119. This compound is primarily utilized in research focused on type 2 diabetes and dyslipidemia, contributing to a better understanding of metabolic regulation and potential therapeutic interventions. Its ability to activate GPR119 makes it a valuable tool for exploring signaling pathways and metabolic processes influenced by this receptor. -
GPR119 Agonists
GPR119 Agonist 2 is an orally active compound targeting the GPR119 receptor, known for its role in glucose metabolism. This reagent demonstrates favorable pharmacokinetic properties in rodent models and effectively enhances glucose tolerance in both mice and rats. GPR119 Agonist 2 is valuable for research focused on type 2 diabetes and metabolic disorders. -
GPR119 Agonist
AS-1669058 free base is a potent agonist of the GPR119 receptor, making it a candidate for diabetes treatment. It stimulates insulin secretion in response to elevated glucose levels both in vitro and in vivo, enhancing insulin promoter activity. In preclinical studies, AS-1669058 demonstrated the ability to improve glucose tolerance and lower blood glucose levels in db/db mice, supporting its potential in metabolic research. -
GPR119 Agonist
AS-1669058 is a selective agonist of the GPR119 receptor, showing promise in the management of type 2 diabetes. This compound enhances insulin secretion in response to elevated blood glucose levels both in vitro and in vivo, while also stimulating insulin promoter activity. In studies using db/db mice, AS-1669058 demonstrated significant improvements in glucose tolerance and reductions in blood glucose levels, indicating its potential utility in diabetes research. -
GPR139 Agonist
Zelatriazin is a selective agonist of the GPR139 receptor, exhibiting a potency with an EC50 of 22 nM. This compound is of particular interest in the study of negative symptoms associated with schizophrenia. Its ability to selectively activate GPR139 makes it a valuable tool for exploring the underlying mechanisms of this psychiatric disorder. -
GPR139 Antagonist
LP-471756 is a potent antagonist of the GPR139 receptor, exhibiting an IC50 value of 640 nM. This compound effectively inhibits cAMP production stimulated by LP-360924, making it a valuable tool for researchers investigating GPR139 signaling pathways and related biological processes. Its application extends to studies in neurobiology and metabolic regulation, where GPR139 plays a crucial role. -
GPR139 Agonist
GPR139 agonist-2 is a selective agonist targeting the GPR139 receptor, demonstrating a potent EC50 of 24.7 nM. This compound has shown promising biological activity by rescuing social interaction deficits and ameliorating cognitive impairments in murine models of schizophrenia. GPR139 agonist-2 holds potential for use in antipsychotic drug research and the exploration of novel therapeutic strategies for schizophrenia. -
GPR171 Agonist
MS15203 is a potent and selective agonist of GPR171, a G protein-coupled receptor involved in neuropeptide signaling. This compound is known to enhance food intake and body weight, likely through the stimulation of neuronal activity. Additionally, MS15203 significantly increases the mRNA levels of proSAAS, neuropeptide Y (NPY), and agouti-related peptide (AgRP), making it a valuable tool for research in appetite regulation and metabolic disorders. -
GPR171 Agonist
BigLEN (mouse) is a highly potent and selective agonist of the orphan G protein-coupled receptor 171 (GPR171), demonstrating a Kd of approximately 0.5 nM. This compound is instrumental in modulating biological processes related to food intake and metabolism, making it valuable for research in appetite regulation and metabolic studies. -
GPR35 Antagonist
CID 2745687 is a selective, reversible antagonist of GPR35, exhibiting a binding affinity with a Ki value of 12.8 nM. This compound is valuable for studies investigating the role of GPR35 in various physiological processes and disease states, making it a useful tool in pharmacology and drug discovery research. Its specificity allows for the exploration of GPR35-related signaling pathways and potential therapeutic interventions. -
GPR35 Antagonist
CID1231538 is a potent antagonist of the GPR35 receptor, a member of the G protein-coupled receptors (GPCRs) family. This benzothiazole analog demonstrates selective inhibition, exhibiting no significant activity against rodent orthologs of GPR35. Its unique properties make it a valuable tool for exploring GPR35-related biological pathways and for investigating potential therapeutic applications in diseases where this receptor is implicated. -
GPR35 Agonist
GPR35 Agonist 4 is a selective activator of the GPR35 receptor, exhibiting a potency with an pEC50 value of 5.86. This compound demonstrates significant biological activity in both human and rat models, making it a valuable tool for studying GPR35 signaling pathways. Notably, mutation of the arginine at position 3.36 negates the agonistic effect of GPR35 Agonist 4, underscoring its mechanism of action. This reagent can be utilized in pharmacological research investigating the role of GPR35 in various physiological and pathological processes. -
GPR35 Agonist
YE120 is a potent agonist of the GPR35 receptor, exhibiting an EC50 of 32.5 nM. This compound activates GPR35, which is involved in various physiological processes, including inflammation and metabolic regulation. YE120 is utilized in research applications focused on understanding GPR35 signaling pathways and its potential roles in disease modulation. -
GPR35 Agonist
GPR35 agonist 5 (3,5-dinitro-bisphenol A; compound 6) functions as a weak agonist of the GPR35 receptor. This compound has been shown to induce cell cycle arrest in CHO-S cells at the G1/G0 phase, highlighting its potential role in cell proliferation studies. GPR35 agonist 5 may be useful for research applications focused on understanding GPR35 signaling pathways and their implications in various biological processes. -
Gpr35 Modulator
Gpr35 Modulator 1 is a potent GPR35 modulator, exhibiting an IC50 of ≤ 100 nM in HEK293 cells stably expressing human GPR35. This compound is valuable for investigating the physiological and pathological roles of GPR35 in various biological processes. Research applications include studies on inflammation, metabolic disorders, and gastrointestinal functions, facilitating the exploration of GPR35 as a therapeutic target. -
GPR35 Modulator
Gpr35 modulator 2 is a selective modulator of the GPR35 receptor, which plays a critical role in various physiological processes. This compound is valuable for investigating GPR35-related disorders and elucidating the receptor's role in cellular signaling pathways. It presents a useful tool for researchers studying the pathophysiology associated with GPR35 and exploring potential therapeutic avenues. -
GPR35 Activator
GPR35 activator-1 is a highly potent activator of the GPR35 receptor, exhibiting an inhibition constant (Ki) of 0.08 nM for human GPR35. This compound is valuable for research involving GPR35 signaling pathways, making it applicable in studies of immune response, gastrointestinal function, and neurobiology. Its high potency makes it a useful tool for elucidating the biological roles and therapeutic potential of GPR35 in various physiological and pathological contexts. -
GPR35 Agonist
GPR35 Agonist 3 is a synthetic compound that selectively activates the GPR35 receptor, exhibiting an EC50 value of 1.4 μM. This reagent is valuable for investigating a range of biological mechanisms and disease states, including gastric cancer, type 2 diabetes, cardiovascular disorders, and immune system functions. Researchers can utilize GPR35 Agonist 3 to explore its therapeutic potential and the role of GPR35 in various physiological processes. -
GPR Agonist
ML301 is a small molecule G-protein coupled receptor (GPCR) agonist that activates GPR signaling pathways. This compound exhibits potent biological activity, effectively competing for 125I-NT binding and demonstrating inhibition by SR142948A with an IC50 of approximately 63 nM. ML301 is useful for research applications exploring GPCR mechanisms, signal transduction, and receptor pharmacology. -
GPR35
Diethyl-Lodoxamide is a potent agonist of the GPR35 receptor, demonstrating significant potential for the treatment of inflammatory bowel disease. It activates GPR35 in human, mouse, and rat models, exhibiting similar EC50 values across these species. Notably, Diethyl-Lodoxamide has been shown to alleviate clinical symptoms in DSS-induced mouse models of inflammatory bowel disease, offering a more effective solution compared to traditional therapies such as 5-ASA. The compound's pharmaceutical properties have been carefully optimized to align with advanced drug design requirements. -
GPR39 Agonist
Lithocholic acid 3-sulfate (disodium) is a GPR39 agonist demonstrating robust activation with EC50 values of 0.88 μM in the presence of Zn2+ and 41 μM in its absence, in relevant cell lines. This compound initiates intracellular calcium signaling through GPR39, not relying on Zn2+-binding sites. Additionally, it functions as a ligand for RORγt, selectively inhibiting Th17 cell differentiation. Lithocholic acid 3-sulfate (disodium) is valuable for investigations into cholestatic liver diseases and related immunological studies. -
GPR39 Agonist
Taurolithocholic acid 3-sulfate disodium is an agonist of the GPR39 receptor, demonstrating EC50 values of 71.6 μM and 69.4 μM in the absence of Zn2+ and 9 μM and 9.6 μM in the presence of Zn2+, as observed in M39-20 and hGPR39-2 cell lines, respectively. This compound activates GPR39 to promote intracellular calcium signaling while functioning independently of Zn2+ binding sites H17 and H19. Taurolithocholic acid 3-sulfate disodium is suitable for investigations related to gallbladder disease and its underlying mechanisms. -
GPR52 Agonist
PW0787 is a potent and selective agonist of the GPR52 receptor, exhibiting an EC50 of 135 nM. This compound demonstrates significant brain penetration and has been shown to effectively suppress psychostimulant behavior. It is valuable for research applications in neuropharmacology and the study of GPR52's role in modulating psychiatric disorders. -
GPR52 Antagonist
GPR52 antagonist-1 is a selective antagonist of the GPR52 receptor, exhibiting an IC50 of 0.63 μM. This compound effectively reduces levels of the mutant huntingtin protein (mHTT) and supports the survival of mouse primary striatal neurons. GPR52 antagonist-1 is important for research applications investigating neurodegenerative disorders, particularly Huntington's disease, and offers insights into the role of GPR52 in neuronal health. -
GPR52 Agonist
NXE0041178 is a potent full agonist of the GPR52 receptor, exhibiting a pEC50 of 7.5 for human GPR52 and an EC50 of 27.5 nM for rat GPR52. This compound demonstrates an ability to penetrate the blood-brain barrier and shows minimal inhibition of hERG, hNaV1.5, and cytochrome P450 isoforms. Notably, NXE0041178 effectively reduces d-amphetamine-induced hyperactivity in rat models, making it a valuable tool for research related to neurological disorders. -
GPR52 Antagonist
GPR52 Agonist-1 is a potent GPR52 agonist with an pEC50 value of 7.53, demonstrating oral bioactivity and the ability to penetrate the blood-brain barrier. This compound enhances cAMP accumulation through direct engagement with the GPR52 receptor. GPR52 Agonist-1 has shown significant efficacy in suppressing methamphetamine-induced hyperactivity in murine models, indicating potential antipsychotic effects. It serves as a valuable tool for research into psychotropic medications and related neurological conditions. -
Metandienone Metabolite
6β-Hydroxy Metandienone is a metabolic derivative of the anabolic androgenic steroid Metandienone, primarily acting as an androgen receptor agonist. This compound exhibits anabolic properties, contributing to muscle growth and strength enhancement. Its biological activity makes it valuable for research in steroid metabolism, performance enhancement, and the study of anabolic steroid effects in various biological systems. -
Estrogen Receptor Antagonist
6-Raloxifene-β-D-glucopyranoside functions as a selective estrogen receptor antagonist, exhibiting a strong affinity for estrogen receptors. This compound is known for its biological activities in inhibiting bone loss and resorption, as well as in reducing lipid levels. It has potential applications in research related to osteoporosis and cardiovascular health, providing insights into estrogen-related metabolic processes. -
Stable Isotope
p,p'-DDE-13C12 is a stable isotope-labeled variant of p,p'-DDE, a well-known metabolite of the persistent pesticide dichlorodiphenyltrichloroethane (DDT). This compound functions as a potent antagonist of the androgen receptor, exhibiting an IC50 value of 5 μM and a Ki of 3.5 μM. p,p'-DDE-13C12 can be utilized in biological research to study endocrine disruption and receptor signaling pathways related to androgen activity. -
Fluticasone Dimer Impurity
Fluticasone dimer impurity is a dimeric form of Fluticasone Propionate, a potent corticosteroid known for its high affinity for glucocorticoid receptors. This impurity may be of interest in investigations related to the stability, purity, and efficacy of Fluticasone formulations. Its assessment can be essential for ensuring quality control in pharmaceutical development and research on corticosteroid activity. -
Abiraterone acetate Degradation Product x
Anhydro abiraterone is a degradation product of Abiraterone acetate, a selective and irreversible inhibitor of CYP17A1, known for its antiandrogen activity. This compound plays a critical role in the study of metabolic pathways and pharmacokinetics of steroidogenesis inhibitors. Research applications include the investigation of androgen receptor signaling and the development of therapeutic strategies for prostate cancer. -
Abiraterone Metabolism
5,6-Dihydroabiraterone is a metabolic derivative of Abiraterone, an irreversible inhibitor of CYP17A1 that exhibits significant antiandrogen effects. This compound plays a crucial role in studying the metabolic pathways of Abiraterone and contributes to understanding its antitumor activity in castration-resistant prostate cancer (CRPC). Research applications include evaluating the pharmacokinetics and metabolic fate of androgen receptor-targeting agents in cancer models. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-1 is a dual inhibitor targeting retinoic acid receptor-related orphan receptor gamma t (RORγt) and dihydroorotate dehydrogenase (DHODH). With IC50 values of 0.083 μM for RORγt and 0.172 μM for DHODH, this compound demonstrates significant potency. RORγt/DHODH-IN-1 has been shown to possess notable in vivo anti-inflammatory activity, making it a valuable tool for research in immunology and inflammation-related studies. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-3 is a dual inhibitor targeting both RORγt and dihydroorotate dehydrogenase (DHODH), exhibiting IC50 values of 0.098 μM for RORγt and 0.432 μM for DHODH. This compound demonstrates significant in vivo anti-inflammatory activity, making it a valuable tool for researchers investigating autoimmune diseases and other inflammatory conditions. Its dual mechanism of action positions it as a promising candidate for therapeutic development in these areas. -
RORγt/DHODH Inhibitor
RORγt/DHODH-IN-2 is a potent dual inhibitor of RORγt and DHODH, targeting key pathways involved in immune regulation and inflammation. This compound exhibits significant biological activity that can be leveraged in the investigation of inflammatory bowel disease (IBD) and related immune disorders. Its dual action provides a valuable tool for research into therapeutic strategies aimed at modulating RORγt and DHODH activity in inflammatory contexts. -
Glucocorticoid/Progesterone Receptor Agoinst
Megestrol is an orally active glucocorticoid and progesterone receptor agonist. It is primarily utilized to stimulate appetite and promote weight gain in patients experiencing anorexia or cachexia, particularly in those with acquired immunodeficiency syndrome (AIDS). Additionally, megestrol may produce effects similar to glucocorticoids and has the potential to elevate the risk of certain mental health disorders. -
Apalutamide Metabolite
Apalutamide-COOH is a metabolite of the androgen receptor antagonist, Apalutamide, which exhibits competitive inhibition with an IC50 of 16 nM. This compound is useful in biological research for studying metabolite activity and its implications in androgen receptor signaling pathways. Its application can aid in understanding the pharmacokinetics and dynamics of Apalutamide in various cellular contexts. -
Abiraterone Metabolite
Abiraterone sulfate is a metabolite of Abiraterone, functioning as a potent and irreversible inhibitor of the CYP17A1 enzyme. This compound exhibits antiandrogen activity, making it significant in the study of androgen receptor signaling pathways. It is primarily utilized in cancer research, particularly for investigating therapies targeting prostate cancer and androgen biosynthesis. -
5α-Reductase Isozyme Inhibitor
Dihydro Dutasteride is a metabolite of Dutasteride, functioning as a potent inhibitor of both isoforms of the 5α-reductase enzyme. This compound exhibits significant biological activity in the modulation of androgen levels, making it valuable for research applications related to prostate health and hair loss disorders. Its inhibitory effects on 5α-reductase facilitate investigations into androgen metabolism and related pathologies. -
Stable Isotope
p,p'-DDE-d8 is a deuterated form of p,p'-DDE, a significant metabolite of the environmental contaminant dichlorodiphenyltrichloroethane (DDT). This compound acts as a potent antagonist of the androgen receptor, exhibiting an IC50 value of 5 μM and a Ki of 3.5 μM. p,p'-DDE-d8 is valuable in biological research for studying receptor interactions and the environmental impact of DDT metabolites on endocrine function. -
Metabolite
Abiraterone sulfate N-oxide is a significant metabolite of Abiraterone, primarily functioning as a carboxylic acid. This compound plays a crucial role in the study of prostate cancer by providing insights into the metabolic pathways and therapeutic effects of Abiraterone. Its biological activity is of interest in research focused on androgen receptor modulation and cancer progression. -
5α-Reductase Isozyme Inhibitor
5β-Dutasteride is a selective inhibitor of both isoforms of 5α-reductase. By inhibiting this enzyme, it effectively reduces the conversion of testosterone to dihydrotestosterone (DHT), making it valuable in studying androgen-related disorders. Its potent biological activity supports research applications in androgen-related conditions, including benign prostatic hyperplasia and androgenetic alopecia. -
Abiraterone Metabolite
Abiraterone N-oxide is a metabolite of Abiraterone, a potent and irreversible inhibitor of CYP17A1. This compound exhibits significant antiandrogen activity, making it valuable for research on prostate cancer and androgen-dependent tumors. Abiraterone N-oxide can be utilized in studies investigating metabolic pathways and resistance mechanisms associated with androgen receptor signaling.
