Catalog No.
Product Name
Application
Product Information
Citations
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Glucocorticoid Receptor Modulator
AL-438 is a selective glucocorticoid receptor modulator that exhibits potent activity with a Ki of 2.5 nM for the glucocorticoid receptor, along with lower affinities for other steroid receptors. This compound demonstrates significant anti-inflammatory properties, making it a valuable tool for research focused on inflammation and endocrine signaling pathways. Its oral bioavailability enhances its utility for in vivo studies in various therapeutic contexts. -
Glucocorticoid Receptor Modulator
Glucocorticoid receptor-IN-2 is a selective modulator of the glucocorticoid receptor (GR) that exhibits significant anti-inflammatory properties. This compound demonstrates notable transcriptional repressive activity with an IC50 of 0.171 nM against human matrix metalloproteinase 1 (hMMP1), while also showing comparable transcriptional activation activity with an EC50 of 0.94 nM against mouse mammary tumor virus (MMTV). It is a valuable reagent for research into GR-mediated pathways and the development of therapies targeting inflammation. -
Stable Isotope
Cortisone-13C3 is a stable isotope-labeled form of cortisone, specifically 13C-labeled at three sites. Cortisone, an oxidized metabolite of cortisol, exhibits anti-inflammatory and immunosuppressive properties through its interaction with the glucocorticoid receptor. This reagent is valuable for research applications in metabolic studies, pharmacokinetics, and the investigation of glucocorticoid signaling pathways in various biological contexts. -
Stable Isotope
Cortisone-d2 is a deuterium-labeled form of cortisone, an oxidized metabolite of cortisol, and a glucocorticoid. This stable isotope serves as a valuable tool for research applications, including metabolic studies and pharmacokinetic analysis. Cortisone exhibits notable immunosuppressive and anti-inflammatory properties, and its interactions with the glucocorticoid receptor can be examined through labeling to enhance the understanding of glucocorticoid dynamics in biological systems. -
Glucocorticoid Receptor Agonist
Tegacorat is a selective glucocorticoid receptor agonist with an EC50 of less than 100 nM. It modulates anti-inflammatory pathways and is valuable in the study of inflammatory diseases, contributing to understanding the underlying mechanisms of glucocorticoid action. This compound serves as a potential lead in developing therapeutic strategies targeting glucocorticoid receptor-mediated responses. -
Glucocorticoid Receptor Agonist
RU26988 is a selective agonist of the glucocorticoid receptor, exhibiting minimal affinity for mineralocorticoid receptors. This compound primarily modulates glucocorticoid signaling pathways, making it a valuable tool for investigating the role of glucocorticoids in various biological processes. Its specificity and activity render RU26988 suitable for research applications in endocrinology, immunology, and inflammation studies. -
Glucocorticoid Receptor
Rofleponide 21-palmitate specifically targets the glucocorticoid receptor, acting as a synthetic glucocorticoid. This compound exhibits potent anti-inflammatory and immunosuppressive properties, making it valuable for research in the fields of immunology and endocrinology. Its selective action allows for the study of glucocorticoid signaling pathways and therapeutic applications in conditions such as asthma and autoimmune diseases. -
GR Antagonist
LLY-2707 is a selective antagonist of the glucocorticoid receptor (GR). It exhibits potential biological activity in mitigating the effects of glucocorticoids, making it a valuable tool for research into diabetes management and the exploration of psychiatric disorders, including schizophrenia. -
GR Activator
Deacylcortivazol is a potent glucocorticoid receptor (GR) activator. It exhibits significant biological activity by modulating GR signaling pathways, which are crucial for various physiological processes, including inflammation and metabolism. This compound is primarily used in research applications that investigate the role of glucocorticoids in cellular responses and their therapeutic potential in inflammatory diseases and stress responses. -
Glucocorticoid
Rofleponide is a synthetic glucocorticoid that selectively binds to glucocorticoid receptors, exhibiting a high affinity for rat thymic receptors. This compound demonstrates significant anti-inflammatory activity in various experimental animal models. It is utilized in research to explore therapeutic pathways for inflammation-related conditions and to study glucocorticoid receptor signaling. -
Glucocorticoid Receptor Agonist
Benzodrocortisone is a glucocorticoid receptor agonist that demonstrates anti-inflammatory properties. It is primarily utilized in research investigating eye diseases, where it may help elucidate the role of glucocorticoids in ocular inflammation and related pathologies. Its action on the glucocorticoid receptor can provide insights into therapeutic approaches for various ocular conditions. -
Glucocorticoid Receptor Antagonist
LY2623091 is a potent glucocorticoid receptor antagonist known for its role in modulating mineralocorticoid signaling. This compound demonstrates significant potential in the treatment of refractory hypertension by inhibiting the action of glucocorticoids, thereby addressing hypertension mechanisms. Additionally, LY2623091 exhibits CYP3A4-dependent clearance, presenting possibilities for synergistic therapeutic strategies when used in conjunction with CYP3A4 inhibitors in research applications. -
Budesonide Impurity
Budesonide impurity C is a known impurity associated with Budesonide, a potent inhaled corticosteroid that acts as an agonist of the glucocorticoid receptor. This impurity may play a role in studying the pharmacological profiles and quality control of Budesonide formulations. It is relevant for research applications involving drug stability, metabolism, and the assessment of therapeutic efficacy in inflammatory conditions. -
GR Ligand
(Rac)-GSK866 is a non-steroidal ligand that targets the glucocorticoid receptor (GR). This compound serves as an important tool for investigating GR functionality by providing insights into ligand binding mechanisms. The crystal structure of (Rac)-GSK866 in complex with the GR ligand-binding domain (PDB: 3E7C) can facilitate the exploration of GR-targeted therapeutic strategies and the development of novel GR modulators. -
Glucocorticoid Receptor Activator
Clobetasone 17-Propionate is a potent glucocorticoid receptor activator. It exhibits anti-inflammatory and immunosuppressive properties, making it valuable in the treatment of various dermatological conditions such as eczema and psoriasis. This compound is widely utilized in research applications focused on studying corticosteroid signaling pathways and their effects on immune responses and skin disorders. -
Glucocorticoid Receptor Control
6b-Hydroxy triamcinolone acetonide is a metabolite of the synthetic corticosteroid triamcinolone acetonide, produced through the action of cytochrome P450 isoforms CYP3A4, CYP3A5, and CYP3A7. This compound primarily targets glucocorticoid receptors, exerting anti-inflammatory and immunosuppressive effects. It serves as a valuable reagent in studies investigating glucocorticoid signaling pathways and corticosteroid metabolism. -
Glucocorticoid Receptor Control
Cortolone, also known as α-Cortolone, functions as a selective modulator of the glucocorticoid receptor. As a metabolite of the steroid hormone cortisol, it exhibits significant biological activity by influencing gene expression and immune response regulation. Cortolone is primarily utilized in research applications focused on studying the mechanisms of glucocorticoid action and its therapeutic implications in inflammatory and autoimmune disorders. -
Anti-glucocorticoid Agent
Roxibolone is an anti-glucocorticoid agent that acts as a potent antagonist of glucocorticoid receptors. This compound is effective in mitigating glucocorticoid-induced catabolism without exhibiting androgenic activity. Roxibolone is utilized in research studies focused on glucocorticoid-related metabolic disorders, providing insight into potential therapeutic approaches in this field. -
Glucocorticoid Receptor Modulator
Triamcinolone Benetonide is a synthetic glucocorticoid receptor modulator that exhibits significant anti-inflammatory properties. This compound is utilized primarily in research related to inflammatory processes and immune response regulation. Its ability to modulate glucocorticoid receptor activity makes it a valuable tool for studying corticosteroid mechanisms and investigating potential therapeutic applications in various inflammatory disorders. -
Glucocorticoid Receptor Control
11β-Hydroxyetiocholanolone is a potent modulator of the glucocorticoid receptor, acting as a metabolite of hydrocortisone. This compound is integral to studying glucocorticoid signaling pathways and their physiological impacts. Its biological activities make it valuable for research applications in endocrinology, stress response mechanisms, and the exploration of glucocorticoid receptor-related disorders. -
Glucocorticoid Receptor Ligand
Win 45164 is an orally active ligand of the glucocorticoid receptor, primarily known for its inhibitory effects on the pituitary-adrenal axis. It promotes liver glycogen deposition and thymus involution in adrenalectomized male rats, highlighting its physiological relevance. Additionally, Win 45164 exhibits significant anti-inflammatory properties, making it a valuable tool for research in inflammatory and neurological diseases. -
Prednisolone Metabolite
20α-Dihydro prednisolone is a metabolite of the corticosteroid prednisolone, primarily targeting glucocorticoid receptors. This compound exhibits anti-inflammatory and immunosuppressive properties, making it valuable for investigating the metabolic pathways of corticosteroids and their effects on inflammation and immune responses. It is useful in research applications related to endocrine disorders and pharmacokinetics of steroid medications. -
Glucocorticoid Receptor Antagonist
N-Demethyl Mifepristone serves as a glucocorticoid receptor antagonist, showing 61% affinity relative to its parent compound Mifepristone. This active metabolite is valuable in research investigating glucocorticoid signaling pathways and their implications in various biological processes. Its capacity to modulate receptor activity makes it a useful tool for studying hormonal regulation and potential therapeutic applications in endocrine disorders. -
Alcoholic Metabolite
22-Hydroxy Mifepristone is a hydroxylated alcoholic metabolite that exhibits both antiprogestational and antiglucocorticoidal activities. This compound contains an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions with azide-containing molecules. With a relative binding affinity of 48% to the human glucocorticoid receptor, 22-Hydroxy Mifepristone serves as a valuable tool for research applications focusing on glucocorticoid signaling and receptor interactions. -
Glucocorticoid Receptor
Prednisolone farnesylate is a transdermal corticosteroid that primarily targets the glucocorticoid receptor. This compound exhibits potent anti-inflammatory activity, making it a valuable tool for research in inflammation and autoimmune responses. Its application includes investigation of glucocorticoid signaling pathways and potential therapeutic effects in inflammatory disorders. -
Glucocorticoid Receptor
Betamethasone 17-benzoate is a potent glucocorticoid receptor agonist. It exhibits anti-inflammatory and immunosuppressive properties, making it effective in the treatment of conditions such as recurrent aphthous ulcers. This compound is valuable for research applications related to corticosteroid mechanisms and therapeutic interventions in inflammatory diseases. -
Glucocorticoid Receptor
Timobesone is a synthetic corticosteroid that primarily targets the glucocorticoid receptor, exhibiting anti-inflammatory and immunosuppressive properties. Although not commercially marketed, it has potential applications in research related to inflammatory skin conditions and immune response modulation. Timobesone's ability to activate glucocorticoid signaling pathways makes it a valuable reagent for investigating corticosteroid effects in biological systems. -
Progesterone Receptor Activator
Cridanimod is a potent activator of the progesterone receptor (PR) that functions primarily through the induction of interferon-alpha (IFNα) and interferon-beta (IFNβ) expression. As a small-molecule immunomodulator and interferon inducer, it plays a crucial role in modulating immune responses. Cridanimod is primarily utilized in research applications focusing on reproductive biology, immunology, and the therapeutic potential of interferon-mediated pathways. -
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. -
NF-κB/AP-1 Inhibitor
Glucocorticoid receptor modulator 1 is a selective non-steroidal modulator that targets the glucocorticoid receptor, exhibiting potent inhibition of NF-κB and AP-1 with IC50 values of 9 nM and 130 nM, respectively. This compound effectively reduces the expression of key inflammatory cytokines, including IL-6, IL-1β, and TNF-α. Additionally, it demonstrates potential in alleviating dermatitis in preclinical models, making it a valuable tool for research in inflammation and immune response. -
Glucocorticoid Receptor Modulator
BMS-791826 is a selective glucocorticoid receptor modulator that targets glucocorticoid receptors to exert its biological effects. This compound effectively inhibits AP-1 and NF-κB-dependent signaling pathways, making it a valuable tool for studying the mechanisms underlying inflammatory diseases. Research applications include the exploration of potential therapeutic strategies for conditions associated with dysregulated glucocorticoid receptor activity. -
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. -
Estrogen Receptor Inhibitor
Indazole-Cl functions as a specific inhibitor of the Estrogen Receptor β, exhibiting anti-inflammatory properties. It effectively impairs the expression of cyclooxygenase-2 induced by hypoxic conditions and reduces reactive oxygen species (ROS) production. Additionally, Indazole-Cl inhibits both cell migration and invasion in response to hypoxia, making it a potent agent against hypoxia-induced inflammation in vascular smooth muscle cells. This compound is valuable for research focusing on estrogen signaling and inflammatory pathways. -
Antiandrogen
RU 59063 is an N-substituted arylthiohydantoin that functions as a potent antiandrogen through its high binding affinity for the rat androgen receptor (Ki: 0.71 nM, rAR). This nonsteroidal compound serves as a valuable radioprobe for studies involving androgen receptor signaling. It is widely utilized in research applications focusing on androgen signaling pathways and related therapeutic targets. -
Thyroid Hormone Receptor Antagonist
DS08210767 is a potent antagonist of the thyroid hormone receptor, exhibiting an IC50 value of 90 nM. This compound effectively inhibits receptor activity, making it a valuable tool for investigating thyroid hormone signaling pathways. Its oral bioavailability enhances its utility in preclinical research focused on thyroid-related disorders and metabolic regulation. -
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.
