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Endocrinology/HormonesGlucocorticoid 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.
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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Corticosterone
Cited
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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CitedFinerenone
T213951050477-31-0
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.
- $31
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Cort108297 Cited
T150001018679-79-2
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).
- $289
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CitedMiricorilant
T333931400902-13-7In house
Miricorilant (CORT 118335) is a selective glucocorticoid receptor modulator for the study of digestive and metabolic disorders.
- $293
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Methylprednisolone succinate Cited
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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CitedDexamethasone Cited
T107650-02-2
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.
- $29
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CitedAZD9567
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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Glucagon (1-29), bovine, human, porcine hydrochloride
T15389L28270-04-4
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.
- $79
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Mifepristone Cited
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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CitedHydrocortisone Cited
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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CitedEplerenone
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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T6876574220-07-8
Spirorenone (INN) is a novel aldosterone antagonist with anti-salt corticosteroid activity, used in metabolic disease research.
- $373
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INCB13739
T60203869974-19-6
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.
- $100
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Prednisone acetate
T8396125-10-0
Prednisone acetate (Prednisone 21-acetate) is a glucocorticoid receptor agonist with immunomodulating properties and anti-inflammatory.
- $41
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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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Fluticasone (propionate)
T018880474-14-2
Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.
- $45
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Corticosterone-d8
TMIH-01671271728-07-4
Corticosterone-d8 is a 2H-labeled corticosteroid, an orally active adrenal corticosteroid with mineralocorticoid and glucocorticoid activity, involved in hormonal regulation in animals.
- $160
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Vamorolone
T1721713209-41-1
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.
- $31
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Spironolactone Cited
T0476
Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.
- $33
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Cited6α-Methylprednisolone 21-hemisuccinate sodium salt
T02942375-03-3
6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone), a water-soluble ester, is used for allergic, cardiac, and hypoxic emergencies.
- $39
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Prednisolone
T156050-24-8
Prednisolone (Hydroretrocortine) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.
- $29
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Prednisolone valerate acetate
T2073472064-79-0
Prednisolone valerate acetate (Lidomex) is a corticosteroid hormone and prodrug with anti-inflammatory and immunosuppressive effects, which is converted to the active form of Prednisolone upon administration and acts by targeting the glucocorticoid receptor.
- $441
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