glucocorticoids

Glucocorticoids receptor agonist 1 (GRA-1) is a highly effective arylpyrazole-based compound that acts as an agonist for the glucocorticoid receptor. GRA-1 exhibits strong anti-inflammatory properties while maintaining insulin secretion function.

Glucocorticoid receptor agonist 2 is a highly effective anti-inflammatory compound, derived from arylpyrazole, that actively binds to and activates the glucocorticoid receptor. This compound exhibits potent anti-inflammatory properties without disrupting insulin secretion.

11β-HSD1-IN-12 is an 11β-HSD1 inhibitor.11β-HSD1-IN-12 is implicated in the conversion of glucocorticoids in vivo and can be used to study metabolic syndrome and obesity.

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

6β-Hydroxy Testosterone, primarily metabolized from testosterone by CYP3A4 and CYP3A5 enzymes, represents 75-80% of testosterone's metabolites. Both cytochrome P450 enzymes, induced by glucocorticoids and various xenobiotics (including drugs and chemical carcinogens), facilitate the metabolism of xenobiotics and certain endobiotics like steroid hormones. However, the biological effects of 6β-hydroxy testosterone remain poorly understood.

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

11-Dehydrocorticosterone is an endogenous mineralocorticoid. It increases Na+/K+-ATPase mRNA expression in vascular smooth muscle cells and inhibits aldosterone action in B. marinus toad bladder tissue in a concentration-dependent manner. 11-Dehydrocorticosterone decreases the sodium/creatine ratio and increases the potassium/creatine ratio in rat urine in a dose-dependent manner in a model of 11β-hydroxysteroid dehydrogenase inhibition induced by carbenoxolone. Chronic administration 11-dehydrocorticosterone increases plasma glucocorticoids levels, body weight gain, and adiposity, as well as induces insulin resistance in mice.

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.

R-HP210 inhibits LPS-induced transcription of several pro-inflammatory genes (IL-1β, IL-6 and COX-2). r-HP210 has an IC50 value of 3.80 μM for NF-κB-mediated bolus trans-suppression. r-HP210 does not induce trans-activation of glucocorticoids (GCs).

11β-HSD1-IN-6 is a potent inhibitor of 11β hydroxysteroid dehydrogenase enzymes (11β-HSDs). These enzymes are responsible for catalyzing the conversion of the active glucocorticoids, corticosterone or cortisol, to their respective inactive forms, 11-dehydrocorticosterone (11-DHC) and cortisone. The compound 11β-HSD1-IN-6 specifically targets and inhibits 11β-HSD-1, effectively modulating the interconversion of these glucocorticoids. [1]

3',4',7-Trihydroxyisoflavone is a soy isoflavone soy glycoside derivative and Cot (Tpl2/MAP3K8) and MKK4 inhibitor with anticancer, antiangiogenic and free radical scavenging properties.3',4',7-Trihydroxyisoflavone enhances memory effects through modulation of cholinergic function and BDNF signaling pathway in mice.3',4',7-Trihydroxyisoflavone can improve skin barrier function impaired by endogenous or exogenous glucocorticoids and can be used in the study of atopic dermatitis. 3',4',7-Trihydroxyisoflavone enhances memory effects by modulating cholinergic function and BDNF signaling pathway in mice. It can improve the skin barrier function impaired by endogenous or exogenous glucocorticoids, and can be used in the study of atopic dermatitis.