Glucocorticoid Receptor Agonist

Fluocinolone is a potent steroid with highly selective glucocorticoid receptor agonist activity. Fluocinolone stabilizes the blood-retinal barrier by enhancing endothelial tight junctions, inhibiting the VEGF pathway and inflammatory factors. Fluocinolone has high lipophilicity, enabling long-term sustained release in the vitreous. Fluocinolone is used in research related to dermatological diseases, diabetic macular edema, uveitis and oral lichen planus.

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC.

Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br is an Drug-linker conjugates for ADC that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs).

Fluocinonide (Vanos) is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders.

Beclometasone dipropionate, the proagent of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate can be used for asthma .

Hydrocortisone acetate (Hydrocortisone 21-acetate) is a corticosteroid used to reduce swelling, itching and pain caused by minor skin irritations or hemorrhoids.

Methylprednisolone acetate, a prednisolone derivative, is a corticosteroid?hormone. Methylprednisolone acetate can relieve pain and swelling that occurs with arthritis and other joint disorders in vivo.

Megestrol is an orally active glucocorticoid and progesterone receptor agonist. Megestrol can alleviate anorexia, cachexia or unexplained significant weight loss associated with acquired immunodeficiency syndrome (AIDS). Megestrol may cause manifestations similar to those of glucocorticoids and increase the risk of mental disorders.

Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury.

GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone.

Amcinonide is an inhibitor of NO release (IC₅₀ = 3.38 nM). Amcinonide inhibits NNC-induced expression of the proinflammatory genes iNOS, TNF-α, and IL-1β in glial cells. Amcinonide reduces the numbers of T6+/Ia+ cells with a concomitant increase in T6+/Ia- cells. Amcinonide induces a selective reduction in expression of Ia antigens. Amcinonide can also be studied in research for eczematous dermatitis.

Cortisone-d₈ is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.

ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC₅₀ of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC₅₀s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.

Dexamethasone acetate (Standard) (Dexamethasone 21-acetate (Standard)) is the analytical standard of Dexamethasone acetate (HY-14648A). This product is intended for research and analytical applications. Dexamethasone acetate (Dexamethasone 21-acetate) is the acetate form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone acetate has a longer duration of action than Dexamethasone. Dexamethasone acetate can accumulate at inflammatory sites, in mouse liver and mouse lung via nanostructured lipid carriers. Dexamethasone acetate can be used to prepare topical formulations for studies related to sensorineural hearing loss, γ-carrageenan-induced paw edema, chronic active hepatitis, pulmonary diseases, and inflammation after vitreoretinal surgery.

Dexamethasone-4,6α,21,21-d₄ is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.

Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages.

Betamethasone valerate (Betamethasone 17-valerate), the 17-valerate ester of Betamethasone, is a topical corticosteroid with anti-inflammatory activity. Betamethasone valerate is used in the treatment of recurrent aphthous stomatitis. Betamethasone valerate inhibits the binding of the radiolabeled glucocorticoid dexamethasone (³H dexamethasone) to human epidermis and mouse skin with IC₅₀s of 5 and 6 nM, respectively.

Dexamethasone (Hexadecadrol) (GMP) is Dexamethasone (HY-14648) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dexamethasone is an agonist of glucocorticoid receptor.

Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.

Triamcinolone acetonide-d₆ is deuterium labeled Triamcinolone acetonide.