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Glucocorticoid Receptor

The 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.

  • Dexamethasone
    T107650-02-2
    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.
    • $29
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  • Osilodrostat
    T4277928134-65-0
    Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).
    • $43
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  • Finerenone
    T213951050477-31-0
    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).
    • $31
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  • Medroxyprogesterone Acetate
    T126171-58-9
    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.
    • $30
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  • Cortodoxone
    T2748152-58-9
    Cortodoxone (11-Desoxycortisol) is a glucocorticoid steroid hormone that is an intermediate in the biosynthesis of cortisol in the adrenal gland.
    • $40
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  • Ciclesonide
    T2526126544-47-6
    Ciclesonide (Alvesco)(RPR251526) is a glucocorticoid used for the treatment of obstructive airway diseases.
    • $44
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  • Nimodipine
    T034366085-59-4
    Nimodipine (BAY-e 9736), a 1, 4-dihydropyridine calcium channel blocker, acts primarily on vascular smooth muscle cells.
    • $40
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  • Cortisone
    T288453-06-5
    Cortisone (17-Hydroxy-11-dehydrocorticosterone) is a corticosteroid with potent glucocorticoid activity.
    • $39
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  • Dexamethasone Phosphate disodium
    T0947L2392-39-4
    Dexamethasone Phosphate disodium (EGP437. Dex-Phos) is a water-soluble form of the synthetic glucocorticoid dexamethasone.
    • $30
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  • Spironolactone
    T047652-01-7
    Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.
    • $33
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  • Triamcinolone acetonide
    T082076-25-5
    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.
    • $29
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  • Mifepristone
    T110284371-65-3
    Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.
    • $37
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  • Corticosterone
    T0948L50-22-6
    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.
    • $41
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  • Apararenone
    T14301945966-46-1In house
    Apararenone (MT-3995) is a receptor antagonist of mineralocorticoid receptor which can be used to treat non-alcoholic steatohepatitis and diabetic nephropathy.
    • $62
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  • Glucocorticoid receptor agonist-1
    T379082166375-82-0In house
    Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].
    • $226
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  • Hydrocortisone
    T161450-23-7
    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.
    • $30
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  • Methylprednisolone succinate
    T223672921-57-5
    Methylprednisolone succinate (Methylprednisolone hemisuccinate) is a synthetic glucocorticoid and is widely used as an anti-inflammatory agent.
    • $38
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  • Betamethasone valerate
    T11632152-44-5
    Betamethasone valerate (Luxiq) is a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions.
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  • (20S)-Protopanaxatriol
    T281034080-08-5
    (20S)-Protopanaxatriol (g-PPT)(g-PPT), a metabolite of ginsenoside, could regulate endothelial cell functions through the estrogen receptor and glucocorticoid receptor.
    • $53
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  • N-Demethyl Mifepristone
    T80652104004-96-8
    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].
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  • AZD9977
    T90221850385-64-6
    AZD9977 is a novel, selective modulator of mineralocorticoid receptor .
    • $135
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  • Fluorometholone Acetate
    T65033801-06-7
    Fluorometholone Acetate (Oxylone acetate) is a synthetic corticosteroid, used in the treatment of steroid responsive inflammatory conditions of the eye.
    • $39
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  • EX-A5386
    T677422452396-89-1
    EX-A5386 (Glucocorticoid receptor modulator-1) is a potent glucocorticoid receptor modulator, IC50/EC50<100nM.
    • $117
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  • Prednisolone disodium phosphate
    T0208125-02-0
    Prednisolone disodium phosphate, a synthetic glucocorticoid, has immunomodulating and anti-inflammatory properties.
    • $30
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  • Megestrol acetate
    T1284595-33-5
    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.
    • $45
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  • Meprednisone
    T65801247-42-3
    Betapar(Meprednisone (Betapar)) is a glucocorticoid and a methylated derivative of prednisone.
    • $32
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  • Deoxycorticosterone acetate
    T303356-47-3
    Deoxycorticosterone acetate (Cortexone acetate) is the 21-acetate derivative of desoxycorticosterone, used for intramuscular injection for replacement therapy of the adrenocortical steroid.
    • $36
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  • Relacorilant
    T167271496510-51-0
    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.
    • $113
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  • Canrenoate potassium
    T30962181-04-6
    Canrenoate potassium (Soldactone) is a synthetic pregnadiene derivative with anti-aldosterone activity.
    • $29
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  • Mometasone furoate
    T153183919-23-7
    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.
    • $39
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  • GW-870086
    T15451827319-43-7
    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).
    • $36
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  • Diflorasone
    T25482557-49-5
    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
    • $36
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  • Dexamethasone acetate
    T09471177-87-3
    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.
    • $45
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  • Hydrocortisone 17-butyrate
    T027013609-67-1
    Hydrocortisone 17-butyrate (Cortisol 17-butyrate) is a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects.
    • $30
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  • GSK9027
    T228181229096-88-1
    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.
    • $54
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  • AZD9567
    T143861893415-00-3
    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.
    • $212
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  • Fludrocortisone acetate
    T1666514-36-3
    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.
    • $47
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  • Fluorometholone
    T3316426-13-1
    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.
    • $40
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  • Hydrocortisone acetate
    T124350-03-3
    Hydrocortisone acetate (Cortisol 21-acetate) is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties.
    • $47
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  • Hydrocortisone aceponate
    T3211474050-20-7
    Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is an effective topical glucocorticoid used in the form of a cream to treat various skin diseases.
    • $39
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  • Fluocinonide
    T6502356-12-7
    Fluocinonide (Topsyn) (Vanos) is an effective glucocorticoid steroid, utilized in the treatment as the skin disorders anti-inflammatory agent.
    • $42
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  • Loteprednol etabonate
    T018182034-46-6
    Loteprednol etabonate (Lotemax) is an ophthalmic analog of the corticosteroid prednisolone with anti-inflammatory activity.
    • $39
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  • Amcinonide
    T026151022-69-6
    Amcinonide (CL-34699) is a Corticosteroid. The mechanism of action of amcinonide is as a Corticosteroid Hormone Receptor Agonist.
    • $35
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  • Eplerenone
    T0083107724-20-9
    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.
    • $44
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  • Fluticasone furoate
    T21404397864-44-7
    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.
    • $30
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  • Dexamethasone palmitate
    T1510214899-36-6
    Dexamethasone palmitate (DXP), a lipophilic prodrug of Dexamethasone, shows a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Dexamethasone palmitate is a glucocorticoid receptor agonist and an anti-inflammatory agent.
    • $43
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  • Velsecorat
    TQ02251196509-60-0
    Velsecorat (AZD7594) is an effective and selective nonsteroidal glucocorticoid receptor modulator (IC50: 0.9 nM).
    • $54
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  • Desonide
    T1168638-94-8
    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.
    • $32
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  • Triamcinolone
    T0798124-94-7
    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.
    • $45
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  • Prednisone
    T101853-03-2
    Prednisone (Dehydrocortisone) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.
    • $30
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