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You are here:Home-Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-Glucocorticoid receptor (GR)

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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.

Cat. No. Product Name CAS No. Information
H9511

GSK9027

 		1229096-88-1

GSK9027 is a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone.
H9454

Dazucorilant

 		1496508-34-9

Bofelisimer is a novel potent,selective glucocorticoid receptor antagonist with Ki of 0.28 nM.
H9329

AZD-5423

 		1034148-04-3

AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.
H5782

PF-04308515

 		1206876-95-0

PF-04308515 (PF 4308515) is a potent glucocorticoid receptor (GR) agonist with anti-inflammatory activity.
H5781

ORIC-101

 		2222344-98-9

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.
H5780

Mapracorat

 		887375-26-0

Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM; does not show significant activity for ERα, PR, AR or MR; shows anti-inflammatory efficacy after topical application similar to the classical glucocorticoids, with a better safety profile.
H5779

Loteprednol etabonate

 		82034-46-6

Loteprednol etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.
H5778

LLY-2707

 		1621865-33-5

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.
H5777

JTP-117968

 		2250132-99-9

JTP-117968 is a novel orally available, selective glucocorticoid receptor modulator (SGRM) with IC50 of 6.8 nM; shows highly selective and GR binding affinity, has neither agonist nor antagonist activity against MT receptors; exhibits improved transrepression/transactivation dissociation not only in in vitro assays, but also in in vivo mice experiments.
H5776

Fosdagrocorat

 		1044535-58-1

Fosdagrocorat (PF 04171327) is an orally available, potential dissociated agonist of the glucocorticoid receptor (GR) for the treatment of rheumatoid arthritis, the phosphate ester prodrug of PF-00251802 (dagrocorat).

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