Glucocorticoid receptors

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  1. Fluticasone propionate is a high affinity, selective glucocorticoid receptor agonist (Kd = 0.5 nM).
  2. Ursolic acid(Malol) is a pentacyclic triterpene acid, used in cosmetics, that is also capable of inhibiting various types of cancer cells by inhibiting the STAT3 activation pathway and human fibrosarcoma cells by reducing the expression of matrix metalloproteinase-9 by acting through the glucocorticoid receptor.
  3. Hydrocortisone is a steroid hormone or glucocorticoid produced by the adrenal gland.
  4. GLI antagonist

    GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
  5. Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
  6. Levonorgestrelis a synthetic progesterone analog; binds to the progesterone receptor (relative binding affinities are < 0.02, 7.5, 17, 58 and 323 % for estrogen receptors, glucocorticoid receptors, mineralocorticoid receptors, androgen receptors and progesterone receptors respectively).
  7. glucocorticoid receptor agonist

    Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.
  8. nonsteroidal glucocorticoid receptor agonist

    AZD5423 is a novel nonsteroidal glucocorticoid receptor agonist.
  9. glucocorticoid receptor agonist

    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
  10. progesterone receptor agonist

    Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
  11. glucocorticoid receptor agonist

    Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
  12. synthetic glucocorticoid receptor agonist

    Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation.
  13. Glucocorticoid Receptor Activator

    Glucocorticoid Receptor Activator 1 is a phenyl aziridine precursor that selectively activates the glucocorticoid receptor (GR). This compound down-regulates TNF-induced pro-inflammatory gene expression, making it a valuable tool for studying inflammation mechanisms. Its role in modulating inflammatory responses positions it as an important reagent for research in various inflammatory conditions.
  14. Endogenous Glucocorticoids

    Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect.
  15. 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.
  16. Prednisolone hemisuccinate is a synthetic glucocorticoid derivative of cortisol, commonly used in the treatment of inflammatory and autoimmune disorders. It exerts anti-inflammatory and immunosuppressive effects by modulating gene expression through glucocorticoid receptor activation.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. Glucocorticoid receptor agonist

    Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
  44. Prednisolone is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
  45. GR antagonist

    AL082D06 is a nonsteroidal glucocorticoid receptor antagonist.
  46. Glucocorticoid receptor antagonist

    The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.
  47. glucocorticoid receptor agonist

    Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.
  48. glucocorticoid agonist

    Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone.
  49. glucocorticoid

    Fluorometholone is a glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders.
  50. Cortisone is a naturally occurring glucocorticoid. It has been used in replacement therapy for adrenal insufficiency and as an anti-inflammatory agent. Cortisone itself is inactive. It is converted in the liver to the active metabolite HYDROCORTISONE.

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