Glucocorticoid Receptor (GR, or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind. The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response. When the glucocorticoid receptor binds to glucocorticoids, its primary mechanism of action is the regulation of gene transcription. The unbound receptor resides in the cytosol of the cell. After the receptor is bound to glucocorticoid, the receptor-glucorticoid complex can take either of two paths. The activated GR complex up-regulates the expression of anti-inflammatory proteins in the nucleus or represses the expression of pro-inflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus. Dexamethasone is an agonist, and RU486 and cyproterone acetate are antagonists of the GR. Also, progesterone and DHEA have antagonist effects on the GR.
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Benzodrocortisone is a synthetic glucocorticoid corticosteroid.
ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity; dose-dependently reduces the expression levels of two established GR target genes, GILZ and FKBP5 with IC50 of 24.9 and 19.5 nM in human PBMCs; demonstrates in vivo antitumor activity by enhancing response to chemotherapy in the GR+ OVCAR5 ovarian cancer xenograft model.
Exicorilant (CORT125281, CORT-125281) is a potent, selective glucocorticoid receptor (GR) antagonist, exhibits no cross-reactivity for the PR and AR receptors.
AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β; demonstrates cell potentcy with IC50 of 55 nM (repression of AP-1 dependent transcription), inhibits LPS-stimulated TNF-α production in human PBMC with IC50 0.43 nM; potently inhibits lung edema in a rat model of allergic airway inflammation with inhaled EC50 of 130 uM/Kg.
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
LLY-2707 (LLY 2707, LLY2707) is a novel potent, selective, nonsteroidal glucocorticoid receptor antagonist with Ki of 2.13 nM; shows substantially lower potency at the other steroid receptors (AR, MR and PR); suppress amphetamine-induced increases in locomotor activity, reduces atypical antipsychotic-associated weight gain in rats.
AZD-9567 is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
AZD-9567 monohydrate is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
Cortisone acetate (Cortisone 21-acetate) is a synthetic glucocorticoid corticosteroid and corticosteroid ester; the C21 acetate ester of cortisone and acts as a prodrug of cortisone in the body.
Prednisolone is a glucocorticoid with the general properties of the corticosteroids.
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