Glucocorticoid Receptor

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and an IL receptor modulator. Dexamethasone has anti-inflammatory and immunosuppressive activity and induces autophagy. Dexamethasone inhibits LPS-induced inflammatory responses in macrophages.

Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).

Finerenone (BAY-948862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone (BAY-948862) displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

Cortodoxone (11-Desoxycortisol) is a glucocorticoid steroid hormone that is an intermediate in the biosynthesis of cortisol in the adrenal gland.

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

Cortisone (17-Hydroxy-11-dehydrocorticosterone) is a corticosteroid with potent glucocorticoid activity.

Nimodipine (BAY-e 9736), a 1, 4-dihydropyridine calcium channel blocker, acts primarily on vascular smooth muscle cells.

Ciclesonide (Alvesco)(RPR251526) is a glucocorticoid used for the treatment of obstructive airway diseases.

Dexamethasone Phosphate disodium (EGP437. Dex-Phos) is a water-soluble form of the synthetic glucocorticoid dexamethasone.

Triamcinolone acetonide (Azmacort) is a Corticosteroid. The mechanism of action of triamcinolone acetonide is as a Corticosteroid Hormone Receptor Agonist. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Miricorilant (CORT 118335) is a selective glucocorticoid receptor modulator for the study of digestive and metabolic disorders.

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

Apararenone (MT-3995) is a receptor antagonist of mineralocorticoid receptor which can be used to treat non-alcoholic steatohepatitis and diabetic nephropathy.

Canrenoate potassium (Soldactone) is a synthetic pregnadiene derivative with anti-aldosterone activity.

Amcinonide (CL-34699) is a Corticosteroid. The mechanism of action of amcinonide is as a Corticosteroid Hormone Receptor Agonist.

Medrysone (6α-Methyl-11β-hydroxyprogesterone) is a topical, synthetic glucocorticoid with metabolic, anti-inflammatory and anti-allergic properties. Medrysone exerts its effect by interacting with specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions is accomplished.

Hydrocortisone (Cortisol) is a glucocorticoid hormone secreted by the adrenocortex. Hydrocortisone agonizes the glucocorticoid receptor, which promotes proteolytic metabolism, gluconeogenesis, capillary wall stabilization, and renal calcium excretion, as well as suppressing immune and inflammatory responses.

N-Demethyl Mifepristone (RU 42633), an active metabolite of Mifepristone, exhibits 61% of the affinity for the glucocorticoid receptor relative to Mifepristone's 100% [1].

AZD9977 is a novel, selective modulator of mineralocorticoid receptor .

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

Hydrocortisone Valerate (Westcort) has anti-inflammatory, antipruritic and vasoconstrictive properties.

Betamethasone (NSC-39470), a glucocorticoid steroid, has immunosuppressive and anti-inflammatory properties.

Ecdysone is a major steroid hormone in insects and herbs. Ecdysone triggers mineralocorticoid receptor activation and induces cellular apoptosis. Ecdysone signaling through Ecdysone receptor isoform B1 is required cell autonomously for the muscle death.

EX-A5386 (Glucocorticoid receptor modulator-1) is a potent glucocorticoid receptor modulator, IC50/EC50<100nM.

Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm

Betapar(Meprednisone (Betapar)) is a glucocorticoid and a methylated derivative of prednisone.

Dexamethasone acetate (NSC 39471) is the acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.

Prednisolone disodium phosphate, a synthetic glucocorticoid, has immunomodulating and anti-inflammatory properties.

GW-870086 is an effective anti-inflammatory agent. GW-870086 also plays a role in a glucocorticoid receptor agonist (pIC50: 10.1 in A549 cells expressing NF-κB).

(20S)-Protopanaxatriol (g-PPT)(g-PPT), a metabolite of ginsenoside, could regulate endothelial cell functions through the estrogen receptor and glucocorticoid receptor.

Betamethasone valerate (Luxiq) is a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions.

Deoxycorticosterone acetate (Cortexone acetate) is the 21-acetate derivative of desoxycorticosterone, used for intramuscular injection for replacement therapy of the adrenocortical steroid.

Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Relacorilant is a selective and orally bioavailable antagonist of glucocorticoid receptor(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.

Methylprednisolone succinate (Methylprednisolone hemisuccinate) is a synthetic glucocorticoid and is widely used as an anti-inflammatory agent.

Mometasone furoate (Sch32088) is a pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.

Hydrocortisone 17-butyrate (Cortisol 17-butyrate) is a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects.

GSK9027 (GR agonist 23a) is a nonsteroidal glucocorticoid receptor (GR) agonist.GSK9027 is a partial agonist on the 2×GRE reporter gene compared to dexamethasone and is less active than dexamethasone activity.

Fluorometholone (Fluoromethalone) is a corticosteroid, most often used after laser-based refractive surgery. It is marketed under the brand names FML (Allergan) and Flarex (Alcon). Fluorometholone acetate ophthalmic suspension is indicated for use in the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the eye.

Fludrocortisone acetate (9α-Fludrocortisone acetate) , a glucocorticoid-receptor agonist, binds to cytoplasmic receptors, translocates to the nucleus, and subsequently initiates the transcription of glucocorticoid-responsive genes such as lipocortins to inhibit phospholipase A2 (PLA2). Fludrocortisone acetate is the acetate salt of a synthetic fluorinated corticosteroid with anti-inflammatory and antiallergic activities. Inhibition of PLA2 activity prevents the release of arachidonic acid, a precursor of eicosanoids such as prostaglandins and leukotrienes; eicosanoids are important mediators in the pro-inflammatory response mechanism. As a mineralocorticoid-receptor agonist, this agent stimulates Na+ reabsorption and water retention and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney.

AZD9567 is a potent and orally active and selective non-steroidal glucocorticoid receptor modulator (SGRM) with an IC50 value of 3.8 nM.It has demonstrated excellent efficacy in the Streptococcus cell wall (SCW) reactivation model of joint inflammation.

Hydrocortisone acetate (Cortisol 21-acetate) is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties.

Fluticasone furoate (Avamys) is a synthetic trifluorinated corticosteroid derived from fluticasone with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflammatory, anti-asthmatic activity, and low systemic exposure. Fluticasone furoate can be used as a nasal spray for studies about allergic rhinitis treatment.

Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is an effective topical glucocorticoid used in the form of a cream to treat various skin diseases.

Desonide (Prednacinolone) is a synthetic glucocorticosteroid for topical use, with anti-inflammatory activity. Desonide binds to glucocorticoid receptors in the cytoplasm, and the ligand-receptor complex is translocated as a homodimer into the nucleus, where transcription activation via glucocorticoid response elements within glucocorticoid-responsive genes occur. This agent induces transcription of genes coding for anti-inflammatory proteins, including lipocortin-1, interleukin-10, interleukin-1 receptor antagonist and neutral endopeptidase. Increased synthesis of lipocortin-1 has an inhibitory effect on phospholipase A2, which in turn inhibits the release of arachidonic acid, thereby controlling the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Velsecorat (AZD7594) is an effective and selective nonsteroidal glucocorticoid receptor modulator (IC50: 0.9 nM).

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.