11β-HSD Substrate

11-Dehydrocorticosterone is an orally active 11β-HSD1 substrate and inactive glucocorticoid. 11-Dehydrocorticosterone is reduced by 11β-HSD1 to the active Corticosterone (HY-B1618). 11-Dehydrocorticosterone drives MR-dependent pro-inflammatory stimulation at low/moderate concentrations and GR-dependent suppression after conversion at high concentrations. 11-Dehydrocorticosterone increases Na,K-ATPase subunit mRNA/protein and pump activity in vascular smooth muscle and aorta. 11-Dehydrocorticosterone induces body weight gain, obesity, hyperinsulinemia, and insulin resistance, and inhibits hypothalamic-pituitary-adrenal axis activity. 11-Dehydrocorticosterone can be used in research on hypertension and metabolic syndrome.

Adamantanone (2-Adamantone; 2-Oxoadamantane) serves as a substrate for some alcohol dehydrogenases and also acts as a probe for characterizing substrate-binding pockets. Adamantanone can be reduced by 3α-hydroxysteroid dehydrogenase and 3β-17β-hydroxysteroid dehydrogenase derived from Pseudomonas testosteroni, and it can fit into the conformationally flexible substrate-binding pockets of these enzymes that undergo substrate-induced fit.

11-Dehydrodexamethasone, Dexamethasone (HY-14648) derivative, is a substrate for 11β-hydroxysteroid dehydrogenase (11β-HSD) 1/2. 11-Dehydrodexamethasone undergoes conversion to Dexamethasone via reductive activity of 11β-HSD.

11-Dehydrocorticosterone-d₁₀ is the d₁₀-labeled 11-Dehydrocorticosterone (HY-113447). 11-Dehydrocorticosterone is an orally active 11β-HSD1 substrate and inactive glucocorticoid. 11-Dehydrocorticosterone is reduced by 11β-HSD1 to the active Corticosterone (HY-B1618). 11-Dehydrocorticosterone drives MR-dependent pro-inflammatory stimulation at low/moderate concentrations and GR-dependent suppression after conversion at high concentrations. 11-Dehydrocorticosterone increases Na,K-ATPase subunit mRNA/protein and pump activity in vascular smooth muscle and aorta. 11-Dehydrocorticosterone induces body weight gain, obesity, hyperinsulinemia, and insulin resistance, and inhibits hypothalamic-pituitary-adrenal axis activity. 11-Dehydrocorticosterone can be used in research on hypertension and metabolic syndrome.

11-Ketoprogesterone (11KP4) is the substrate for CYP17A1 and 11β-HSD2 that could be metabolized to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF) with glucocorticoid activity.

Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC₅₀ of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.