Glucocorticoid Receptor

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.

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.

Finerenone (BAY-948862) is a nonsteroidal antagonist of the mineralocorticoid receptor (MR) (IC50=18 nM) with selective and oral activity. Finerenone is used in the treatment of patients with chronic kidney disease with type 2 diabetes.

Cort108297 is a selective glucocorticoid receptor modulator and a selective GR antagonist with no affinity for other steroid receptors. Cort108297 showed a high affinity for GRs (Ki: 0.45nM).

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

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

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

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.

Glucagon (1-29), bovine, human, porcine hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone produced by pancreatic α-cells that activates HNF4α, increases HNF4α phosphorylation, and stimulates gluconeogenesis.

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

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.

Eplerenone (CGP 30083) is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease.

Spirorenone (INN) is a novel aldosterone antagonist with anti-salt corticosteroid activity, used in metabolic disease research.

INCB13739 is an orally active, selective, and highly efficient 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. INCB13739 improves hyperglycemia in patients with uncontrolled type 2 diabetes on metformin monotherapy and can be used in hyperlipidemia and hypertriglyceridemia research.

Prednisone acetate (Prednisone 21-acetate) is a glucocorticoid receptor agonist with immunomodulating properties and anti-inflammatory.

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.

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

TPI-1 is a SHP-1 inhibitor.

Corticosterone-d8 is a 2H-labeled corticosteroid, an orally active adrenal corticosteroid with mineralocorticoid and glucocorticoid activity, involved in hormonal regulation in animals.

Vamorolone (VBP15) is an orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone displays effective NF-κB inhibition and substantially decreases hormonal effects.

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

6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone), a water-soluble ester, is used for allergic, cardiac, and hypoxic emergencies.

Prednisolone (Hydroretrocortine) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.

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.

Hydrocortisone hemisuccinate (hydrocortisone 21-hemisuccinate*free acid) is a corticosteroid used as an analytical and chromatography reagent.

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

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

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

Halcinonide (Halciderm), a high-efficiency corticosteroid, is served as an anti-inflammatory agent used in topical preparations.

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

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

Mometasone furoate (Sch32088) is a pregnadienediol derivative with anti-allergic and anti-inflammatory properties, used in the management of asthma and allergic rhinitis, as well as a topical treatment for skin disorders.

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

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

Actriol (Epiestriol) is always used as Glucocorticoid Receptor agonist.

Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.

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.

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 Dipropionate is the 17, 21-dipropionate ester of betamethasone, a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions. Betamethasone dipropionate (SCH 11460) binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.

Flumethasone (RS-2177) is a glucocorticoid receptor agonist, with anti-inflammatory, antipruritic and vasoconstrictive properties.

Esaxerenone (XL-550) is a highly potent and selective non-steroidal antagonist of the mineralocorticoid receptor.

Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Clobetasol Propionate is the propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2.

Beclometasone dipropionate (Vancenase) is the dipropionate ester of a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production.

Fluocinonide (Topsyn) (Vanos) is an effective glucocorticoid steroid, utilized in the treatment as the skin disorders anti-inflammatory agent.

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.

Canrenone (SC14266) is an aldosterone antagonist with potassium-sparing diuretic activity.

Budesonide (Pulmicort), an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.