Cortisol and other glucocorticoids bind to the glucocorticoid receptor (GR, or GCR), also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1). The GR regulates the genes that control development, metabolism, and immune response and is expressed in almost all body cells. The regulation of gene transcription is the main mechanism by which the glucocorticoid receptor functions when it binds to glucocorticoids.The cell's cytosol is home to the unbound receptor. The receptor-glucocorticoid complex can proceed in one of two ways after the glucocorticoid and receptor are bound together. By preventing other transcription factors from moving from the cytosol into the nucleus, the activated GR complex controls the expression of anti-inflammatory proteins in the nucleus or suppresses the expression of pro-inflammatory proteins in the cytosol. Dexamethasone is an agonist, while cyproterone acetate and RU486 are GR antagonists. Progesterone and DHEA have opposing effects on the GR as well.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V77401 | (-)-ZK 216348 | (-)-ZK 216348 is the enantiomer of (+)-ZK 216348. | ||
V2896 | AL082D06 | 256925-03-8 | AL082D06 (formerly known as D-06), is a nonsteroidal glucocorticoid receptor (GR) antagonist which is characterized by a tri-aryl methane core chemical structure. | |
V4249 | AZD2906 | 1034148-15-6 | AZD2906 is a novel, potent and selective glucocorticoid receptor (GR)agonist which increases micronucleated immature erythrocytes in the bone marrow of rats. | |
V4250 | AZD5423 | 1034148-04-3 | AZD5423 is the first clinical candidate that displayed a potent inhibition of lung edema in a rat model of allergic airway inflammation following dry powder inhalation combined with a moderate systemic GR-effect, assessed as thymic involution. | |
V4246 | AZD7594 | 1196509-60-0 | AZD7594 (also known as AZ13189620) is a novel, potent selective nonsteroidal indazole ether-based glucocorticoid receptor modulators (SGRMs)with anIC50of 0.9 nM. | |
V77210 | Betamethasone-d5 (Betamethasone d5) | Betamethasone-d5 is the deuterium labelled form of Betamethasone. | ||
V79082 | Flunisolide-d6 (flunisolide d6) | Flunisolide-d6 is the deuterium labelled form of Flunisolide. | ||
V4929 | GW-870086 | 827319-43-7 | GW-870086 is a novel and potent glucocorticoid receptor agonist that has anti-inflammatory properties, and thus can be potentially usef for the treatment of asthma and atopic dermatitis. | |
V14975 | Mapracorat | 887375-26-0 | Mapracorat, formerly known as BOL-303242-X and ZK-245186, is an selective glucocorticoid receptor agonists (SEGRAs) under clinical trials for the topical treatment of atopic dermatitis, inflammation following cataract surgery, and allergic conjunctivitis. | |
V4259 | Mizacorat (AZD9567) | 1893415-00-3 | AZD9567 is a novel, potent, oral bioactive, non-steroidal andselective glucocorticoid receptor modulator (SGRM)with anIC50of 3.8 nM. | |
V80806 | Mometasone furoate-d3 (Sch32088-d3) | Mometasone furoate-d3 is a deuterium-labeled Mometasone furoate. | ||
V79213 | Prednisone acetate-d3 (Prednisone 21-acetate-d3) | Prednisone acetate-d3 is the deuterated form of Prednisone acetate. | ||
V79709 | Prednisone-d8 (Dehydrocortisone-d8) | Prednisone-d8 is the deuterium labelled form of Prednisone. | ||
V18495 | Clobetasone Butyrate | 25122-57-0 | Clobetasone Butyrate (SN203; Emovate; SN-203;Eumovate; Cloptison;Molivate), the 17-O-butyl ester ofClobetasone, is a corticosteroidthat has been used in dermatology for the treatment of skin inflammation such as eczema, psoriasis. | |
V12358 | Beclometasone (Beclometasone) | 4419-39-0 | Beclomethasone (also called Beclometasone) is a topically used anti-inflammatory corticosteroid used in treatment of asthma and rhinitis. | |
V32506 | Desisobutyryl-ciclesonide (CIC-AP; Ciclesonide active principle) | 161115-59-9 | Desisobutyryl-ciclesonide is the bioactive metabolite of Ciclesonide. | |
V8386 | Cortisone | 53-06-5 | Cortisone is a potent and naturally occurring glucocorticoid with anti-inflammatory activities. | |
V6227 | Dexamethasone Phosphate disodium | 2392-39-4 | Dexamethasone Phosphate disodium, thewater-soluble salt form of dexamethasoneadministeredthrough i. | |
V21144 | Fluorometholone | 426-13-1 | Fluorometholone (also known as NSC 47438)is a synthetic corticosteroid, commonly used as eye dropsin the treatment of steroid responsive inflammatory conditions of the eye. | |
V31047 | Methylprednisolone succinate | 2921-57-5 | Methylprednisolone succinate (Standard) is the analytical standard for Methylprednisolone succinate. |