Catalog No.
Product Name
Application
Product Information
Citations
-
GR Agonist
Flumethasone is a highly selective and potent glucocorticoid receptor (GR) agonist. It effectively activates GR, leading to the inhibition of nuclear factor kappa B (NF-κB) and subsequent reduction of pro-inflammatory cytokine production, such as TNF-α and IL-1β. Additionally, Flumethasone upregulates anti-inflammatory gene expression, particularly IL-10, and modulates metabolic enzyme activity, including tyrosine aminotransferase. This compound is valuable for research into inflammatory diseases, cancer, and endocrine regulation. -
hTNFa Antibody-GC Conjugate
Glucocorticoid receptor agonist-4 Ala-Ala-Mal is a conjugate of an anti-human TNFα antibody and a glucocorticoid receptor agonist. This compound is designed to selectively target and activate glucocorticoid receptors, demonstrating significant anti-inflammatory properties. It is primarily utilized in research focused on autoimmune and inflammatory diseases, enabling in-depth studies of immune response modulation and therapeutic interventions. -
hTNFa Antibody-GC Conjugate
Glucocorticoid receptor agonist-3 Ala-Ala-Mal is a conjugate of a human TNFα antibody and a glucocorticoid receptor agonist. This compound is designed to modulate the immune response, exhibiting anti-inflammatory properties that are relevant in the study of autoimmune and inflammatory diseases. Its application offers valuable insights into therapeutic strategies targeting TNFα, enhancing the understanding of its role in various pathological conditions. -
Glucocorticoid Receptor Agonist
Amcinonide is a glucocorticoid receptor agonist that exhibits anti-inflammatory properties by inhibiting nitric oxide (NO) release with an IC50 of 3.38 nM. It effectively downregulates the expression of pro-inflammatory genes such as iNOS, TNF-α, and IL-1β in glial cells. Moreover, Amcinonide alters T cell populations by reducing T6+/Ia+ cells while increasing T6+/Ia- cells, leading to a selective decrease in Ia antigen expression. This compound is applicable in research related to eczematous dermatitis and the modulation of inflammatory responses. -
Glucocorticoid Receptor Agonist
Fluocinolone (Acetonide) is a glucocorticoid receptor agonist that exhibits significant anti-inflammatory and anti-lipid accumulation effects. It promotes the proliferation of dermal papilla cells (DPCs) and shows potential in the repair of injured pulp tissues. This compound is also valuable in research focused on mitigating chemotherapy-induced peripheral neuropathy associated with Paclitaxel. -
SHRs Agonist
Triamcinolone is a long-acting corticosteroid that acts as a glucocorticoid receptor agonist. It exhibits multiple biological activities, including anti-inflammatory, anti-oedematous, anti-proliferative, anti-angiogenic, immunomodulatory, and neuroprotective effects. This compound is widely utilized in research for the treatment of various dermatological conditions, immune disorders, and ocular diseases. -
Mineralocorticoid/Glucocorticoid Receptor Agonist
Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. It exhibits significant anti-inflammatory properties by suppressing pro-inflammatory cytokine expression, including CCL2, IL-6, and IL-8 levels, while enhancing renal sodium and water transport, which contributes to increased plasma volume and blood pressure. Additionally, fludrocortisone induces key signaling pathways such as PI3K/Akt, mTOR, and ERK1/2, and is utilized in research applications related to congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency. -
GR/IL-6 Inhibitor
Glucocorticoid receptor/IL-6-IN-1 is a selective dual inhibitor that targets both the glucocorticoid receptor (GR) and the IL-6 signaling pathway, demonstrating IC50 values of 120 nM and 59 nM, respectively. This compound effectively inhibits IL-6-induced phosphorylation of JAK/STAT3, thereby blocking the transcription of inflammatory cytokines. Glucocorticoid receptor/IL-6-IN-1 is a valuable tool for investigating inflammatory diseases, including rheumatoid arthritis and asthma. -
Glucocorticoid Receptor Activator
Flunisolide hemihydrate is an orally active glucocorticoid receptor activator with potent anti-inflammatory properties. It induces eosinophil apoptosis, making it a valuable tool for researchers investigating asthma, rhinitis, and various inflammatory conditions. Its mechanism of action supports studies focused on the modulation of inflammatory pathways and the therapeutic applications of corticosteroids in respiratory diseases. -
Stable Isotope
Dexamethasone-4,6α,21,21-d4 is a deuterated derivative of Dexamethasone, functioning as a glucocorticoid receptor agonist. It exhibits potent anti-inflammatory properties, including the modulation of neutrophil and monocyte surface markers such as CD11b and CD18, which are crucial for immune cell activation and migration. This reagent is particularly relevant for research on inflammatory responses, including studies related to COVID-19, as well as investigations into exosome-mediated microRNA regulation in macrophage activation. -
Stable Isotope
Dexamethasone-d5 is a deuterium-labeled analog of the glucocorticoid receptor agonist Dexamethasone. It is known to reduce the expression of CD11b, CD18, and CD62L on neutrophils, as well as CD11b and CD18 on monocytes, thereby modulating immune responses. This stable isotope is particularly valuable in research applications studying the mechanics of inflammation, including the regulation of exosomal microRNA-155 production in lipopolysaccharide-stimulated macrophages, and its efficacy in managing conditions such as COVID-19. -
Stable Isotope
Dexamethasone-d4 is a deuterium-labeled derivative of Dexamethasone, which acts as a potent glucocorticoid receptor agonist. This compound has notable biological activities, including the modulation of immune cell marker expression by decreasing levels of CD11b, CD18, and CD62L on neutrophils, as well as CD11b and CD18 on monocytes. Dexamethasone-d4 is particularly valuable for research applications related to anti-inflammatory responses and the investigation of COVID-19 pathophysiology, as it inhibits exosome production containing inflammatory microRNA-155 during macrophage activation. -
Glucocorticoid Receptor Ligand
PF-04308515 is a selective glucocorticoid receptor ligand that exhibits significant anti-inflammatory properties. It effectively inhibits the production of interleukin-6 (IL-6) and interferon gamma (IFNγ), making it a valuable tool for studying inflammation and immune responses. Additionally, PF-04308515 induces a weak interaction with PGC1α, providing insights into its potential metabolic effects. This compound is useful for research applications focused on inflammation, autoimmune diseases, and glucocorticoid signaling pathways. -
GR/IL-6 Inhibitor
Glucocorticoid receptor/IL-6-IN-2 is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and the IL-6 signaling pathway, with IC50 values of 40 nM and 19 nM, respectively. This compound has demonstrated significant potential in inhibiting inflammatory responses, making it a valuable tool for research into inflammatory diseases such as rheumatoid arthritis and asthma. Its unique mechanism of action allows for exploration of therapeutic strategies aimed at modulating immune responses and mitigating chronic inflammation. -
Stable Isotope
Mifepristone-d6 is a deuterated form of Mifepristone, a potent antagonist of the progesterone receptor (PR) and the glucocorticoid receptor (GR), exhibiting IC50 values of 0.2 nM and 2.6 nM, respectively, in in vitro assays. This stable isotope-labeled compound serves as a valuable tool for metabolic studies, pharmacokinetic investigations, and research on receptor interactions. Its unique isotopic signature allows for precise tracking and analysis in biological systems, facilitating advanced research in endocrinology and reproductive health. -
Glucocorticoid Receptor Agonist
Beclometasone dipropionate monohydrate is a potent glucocorticoid receptor agonist with significant anti-inflammatory properties. It functions through the activation of the glucocorticoid receptor, effectively suppressing inflammation and cellular hyperproliferation. This compound is primarily utilized in research related to asthma treatment and the modulation of inflammatory responses. -
Drug-Linker Conjugate for ADC
Glucocorticoid receptor modulator 4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications. This compound demonstrates glucocorticoid receptor (GRE) reporter activation in mTNF-expressing K562 cells with an EC50 of 40 μM. Additionally, it exhibits binding affinity with anti-tumor necrosis factor (TNF) antibodies and exhibits anti-inflammatory effects in mouse models of arthritis, making it a valuable tool for research in inflammation and autoimmune diseases. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Mal is a glucocorticoid receptor agonist designed for targeted drug delivery applications. This compound functions as a linker in antibody-drug conjugates (ADCs) and facilitates the synthesis of anti-CD40 antibody conjugates for therapeutic research. Its modulation of glucocorticoid receptor activity makes it valuable for studies investigating immune response and inflammation targets. -
FKBP51 Degrader, VHL Binder
SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity. -
Glucocorticoid Receptor Agonist
Glucocorticoid Receptor Agonist-1 is a highly potent glucocorticoid receptor agonist with an IC50 of 2.8 nM. This compound modulates the glucocorticoid receptor, influencing a variety of physiological processes including inflammation and immune responses. It is suited for research applications aimed at exploring mechanisms of glucocorticoid signaling and its implications in diseases such as asthma, arthritis, and other inflammatory conditions. -
GR Agonist
Glucocorticoid receptor agonist-2 is a potent agonist of the glucocorticoid receptor (GR) with an IC50 value of 6.6 nM. This compound is instrumental in synthesizing anti-inflammatory antibody-drug conjugates (ADCs), making it valuable for research in inflammation and immune response modulation. Its effectiveness as an active reference in studies related to GR-targeted therapies supports its applicability in therapeutic development. -
Glucocorticoid Receptor Agonist
Glucocorticoid Receptor Agonist-5 is a potent agonist of the glucocorticoid receptor. This compound exhibits significant anti-inflammatory and immunosuppressive properties, making it valuable in research focused on inflammatory diseases and immune response modulation. Additionally, it serves as an antibody-drug conjugate (ADC) cytotoxin, facilitating targeted therapeutic approaches in cancer research. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-4 is a selective agonist for the glucocorticoid receptor, offering insights into the modulation of inflammatory processes. This compound can be conjugated to TNF-α antibodies, facilitating research into autoimmune and inflammatory diseases. Its applications extend to the study of glucocorticoid signaling pathways and therapeutics in related conditions. -
Glucocorticoid Receptor Agonist
Glucocorticoid Receptor Agonist-3 is an effective agonist that targets the glucocorticoid receptor. It exhibits significant anti-inflammatory and immunomodulatory activities, making it valuable for research in the fields of inflammation, autoimmune diseases, and hormone signaling. This compound is essential for studying the therapeutic potential of glucocorticoids in various biological contexts. -
GR Agonist
Glucocorticoid receptor agonist-6 is a specific agonist for the glucocorticoid receptor (GR). It exhibits significant cytotoxic activity, making it an excellent candidate for use as a payload in the synthesis of antibody-drug conjugates (ADCs). This compound supports research in targeted therapy approaches for diseases where GR modulation is beneficial. -
Stable Isotope
Budesonide-d6 is a deuterium-labeled derivative of Budesonide, primarily targeting the glucocorticoid receptor. Known for its anti-inflammatory properties, Budesonide-d6 is utilized in research to study mechanisms of action related to asthma and lung diseases. This stable isotope variant allows for enhanced tracking of Budesonide pharmacokinetics and dynamics in biological systems, making it valuable for studies focused on tumor reduction and gene expression modulation. -
Drug-Linker Conjugate for ADC
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br functions as a drug-linker conjugate for antibody-drug conjugate (ADC) applications. This compound facilitates the synthesis of various therapeutic agents, including ABBV-154, ABBV-927, and ABBV-368, by effectively targeting the glucocorticoid receptor. Its utility in ADC development makes it a valuable reagent for researchers focused on innovative treatment strategies in oncology and immunology. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-1 Ala-Ala-Mal is a potent agonist of the glucocorticoid receptor, playing a critical role in anti-inflammatory and immunosuppressive pathways. This compound can be strategically conjugated with Adalimumab to develop antibody-drug conjugates (ADCs) for targeted therapy applications. Its functionality makes it a valuable reagent for research in chronic inflammatory conditions and autoimmune diseases. -
ABBV-3373 Reference
Glucocorticoid receptor agonist-2 Ala-Ala-Mal acts as an active reference for ABBV-3373 and serves as a ligand for the glucocorticoid receptor. This compound is instrumental in the synthesis of antibody-drug conjugates (ADCs) with anti-inflammatory properties. Its ability to modulate glucocorticoid receptor activity makes it a valuable reagent in the development of therapeutics targeting inflammatory diseases. -
ADC/PROTAC Linkers
Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br serves as a versatile drug-linker conjugate for antibody-drug conjugate (ADC) applications. This reagent enables the synthesis of conjugates targeting the CD40 antigen, facilitating the development of targeted therapies. Its unique structure supports the design of PROTACs and other innovative bio-conjugates, contributing to advances in cancer research and immunotherapy. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a selective agonist of the glucocorticoid receptor, facilitating the modulation of anti-inflammatory and immunomodulatory pathways. This compound is particularly useful in the development of antibody-drug conjugates (ADCs) targeting the CD40 receptor, offering insights into therapeutic strategies for conditions related to inflammation and immune regulation. It serves as a vital tool for researchers investigating glucocorticoid signaling in various biological contexts. -
Drug-Linker Conjugate
Glucocorticoid Receptor Drug-Linker 1 is a specialized drug-linker conjugate designed for the synthesis of Antibody-Drug Conjugates (ADCs) targeting BDCA2. This compound facilitates precise delivery of therapeutic agents to BDCA2-expressing cells, enhancing the efficacy of treatment while minimizing off-target effects. It is particularly relevant in research focused on immunology and targeted cancer therapies. -
Stable Isotope
Fluocinolone acetonide-13C3 is a stable isotope-labeled form of Fluocinolone, a potent glucocorticoid receptor agonist. It exhibits anti-inflammatory properties and effectively inhibits lipid accumulation, making it valuable for investigating its effects on various biological processes. Fluocinolone acetonide-13C3 can be utilized in research involving the proliferation of dental pulp cells and the potential repair of injured pulp tissues, as well as in studies focused on mitigating chemotherapy-induced peripheral neuropathy, particularly in relation to drugs like Paclitaxel. -
ADC Linker
INX-P is an antibody-drug conjugate (ADC) linker designed for targeting glucocorticosteroids. It facilitates the delivery of cytotoxic agents specifically to cancer cells that express glucocorticoid receptors, enhancing therapeutic efficacy while minimizing systemic toxicity. This linker is particularly useful in research applications focusing on ADC development and targeted cancer therapies. -
ADC Linker
Glucocorticoid receptor agonist-1 phosphate Gly-Glu TFA is a cleavable linker designed for the synthesis of Antibody-Drug Conjugates (ADCs). This compound facilitates targeted drug delivery by linking cytotoxic agents to antibodies, enhancing therapeutic efficacy while minimizing off-target effects. Its ability to be cleaved under specific physiological conditions makes it a valuable tool in the development of precision medicine strategies. -
Glucocorticoid Agonist
BI 653048 is a selective, orally active nonsteroidal glucocorticoid agonist, targeting the glucocorticoid receptor with an IC50 of 55 nM. It inhibits CYP enzyme isoforms including CYP1A2, CYP2D6, CYP2C9, CYP2C19, and CYP3A4, while exhibiting a reduced affinity for the hERG ion channel (IC50 > 30 μM). Additionally, BI 653048 serves as an HCV NS3 protease inhibitor, demonstrating potential for reducing viral loads in hepatitis C virus infections. This compound is valuable in studies related to glucocorticoid signaling and antiviral research. -
Stable Isotope
Fluticasone propionate-d5 is a deuterium-labeled derivative of fluticasone propionate, a potent topical anti-inflammatory corticosteroid. This compound selectively binds to the glucocorticoid receptor, exhibiting an absolute affinity (KD) of 0.5 nM, and demonstrates minimal interaction with other steroid receptors. It is primarily utilized in research involving anti-inflammatory and potential antiviral activities, making it a valuable reagent for studies focused on corticosteroid receptor mechanism and function. -
Dexamethasone-Glucocorticoid Receptor Inhibitor
Collismycin B is a potent inhibitor of the dexamethasone-glucocorticoid receptor, exhibiting an IC50 value of 10 µM. This compound demonstrates notable antimicrobial activity, making it a valuable tool for research in microbial pathogenesis. Additionally, Collismycin B exhibits cytotoxic properties, offering potential applications in cancer research and therapeutic development. -
Metabolite of Hydrocortisone
20β-Dihydrocortisol is a metabolite of Hydrocortisone that acts as a weak endogenous agonist of the glucocorticoid receptor (GR). This compound is generated from Hydrocortisone through the action of carbonyl reductase 1 (CBR1) in an NADPH-dependent process. Its unique properties make 20β-Dihydrocortisol valuable for investigating metabolic disorders such as obesity and its impact on glucocorticoid signaling pathways. -
Glucocorticoid Receptor Antagonist
CP-394531 is a highly selective non-steroidal antagonist of the glucocorticoid receptor (GR), exhibiting a Ki value of 0.1 nM. It demonstrates minimal binding to the androgen receptor (AR) (Ki = 130 nM) and negligible effects on the progesterone receptor and estrogen receptors (ERα, ERβ). CP-394531 effectively inhibits the agonistic effects of Dexamethasone with a Kif of 4.1 nM. This compound is valuable for researching a variety of conditions, including diabetes, obesity, depression, neurodegenerative disorders, glaucoma, and Cushing's disease. -
Nasal Spray
Fluticasone furoate is a synthetic trifluorinated corticosteroid that targets the glucocorticoid receptor with a high affinity (Kd of 0.3 nM). It exhibits significant anti-inflammatory and anti-asthmatic properties while maintaining low systemic exposure. This compound is primarily utilized in the treatment of allergic rhinitis, providing effective relief from nasal inflammation and associated symptoms. -
Anti-Inflammatory Agent
Methylprednisolone aceponate is a glucocorticoid with a specific mechanism of action as a selective glucocorticoid receptor ligand, primarily functioning as an anti-inflammatory agent. It exhibits weak systemic effects, making it particularly useful in the treatment of localized inflammatory conditions. This compound is valuable for research applications targeting eczema and other inflammatory skin disorders, aiding in the understanding of their pathophysiology and potential treatments. -
Glucocorticoid Receptor Antagonist
Cort108297 is a selective glucocorticoid receptor (GR) antagonist with a high affinity, exhibiting a Ki value of 0.45 nM. This compound effectively modulates GR signaling pathways, making it a valuable tool for elucidating the role of glucocorticoids in various biological processes. Research applications may include studies on inflammation, metabolic regulation, and stress response mechanisms. -
Glucocorticoid Metabolism Marker
Tetrahydrocortisone is a corticosteroid and a crucial marker for glucocorticoid metabolism, formed from endogenous glucocorticoids via the enzyme AKR1D1 (5β-reductase). This compound plays a vital role in maintaining glucocorticoid metabolic homeostasis and is regulated by the glucocorticoid receptor (GR). Tetrahydrocortisone is valuable for mechanistic investigations of metabolic diseases, including non-alcoholic fatty liver disease (NAFLD) and type 2 diabetes, and serves as a reliable biomarker for assessing AKR1D1 activity and glucocorticoid metabolic status in vivo. -
GR Agonist
GSK9027 is a non-steroidal agonist of the glucocorticoid receptor (GR), exhibiting partial agonistic activity on the 2×glucocorticoid response element (GRE) reporter system. This compound demonstrates intrinsic activities comparable to dexamethasone, making it a valuable tool for investigating GR-mediated signaling pathways. GSK9027 can be utilized in research applications focused on inflammation, immune response modulation, and drug development related to glucocorticoid therapies. -
Stable Isotope
Cortisone-d8 is a deuterium-labeled derivative of cortisone, a biologically active metabolite of cortisol and a member of the glucocorticoid class. This stable isotope is utilized in metabolic studies and has applications in pharmacokinetic research and the characterization of glucocorticoid receptor interactions. Cortisone exhibits immunosuppressive and anti-inflammatory properties, contributing to its role in a variety of therapeutic applications. -
Glucocorticoid Receptor Agonist
ZK 216348 is a selective nonsteroidal glucocorticoid receptor agonist, exhibiting an IC50 of 20.3 nM. This compound also interacts with progesterone and mineralocorticoid receptors, with IC50 values of 20.4 nM and 79.9 nM, respectively. ZK 216348 demonstrates significant anti-inflammatory properties comparable to those of Prednisolone while minimizing transactivation-related side effects, making it a valuable tool for research in inflammation and related conditions. -
Drug Metabolite
Beclomethasone 17-propionate is a potent glucocorticoid receptor (GR) agonist and an active metabolite of Beclomethasone dipropionate. It demonstrates a higher affinity for the GR, making it more effective in modulating glucocorticoid activity. This compound effectively suppresses cytokine production in lung macrophages associated with chronic obstructive pulmonary disease (COPD), making it valuable for research in inflammation and respiratory disorders. -
Glucocorticoid
Tetrahydrocorticosterone is a glucocorticoid that functions primarily through binding to the glucocorticoid receptor (GR), thus modulating inflammatory responses. It plays a crucial role in the regulation of carbohydrate, protein, and fat metabolism. This compound is naturally produced by the adrenal glands and is extensively utilized in research focusing on inflammation, metabolic disorders, and endocrine function. Its diverse biological activities make it a valuable reagent for studying glucocorticoid signaling pathways and their implications in various physiological and pathological conditions. -
Glucocorticoid
Clobetasone butyrate is a synthetic glucocorticoid that modulates inflammation primarily through its action on glucocorticoid receptors. It exhibits potent topical anti-inflammatory activity, making it effective for treating corticosteroid-responsive dermatoses such as atopic dermatitis and psoriasis. This compound is useful for research focused on skin inflammation and therapeutic approaches to dermatological conditions.
