steroid

Budesonide (Pulmicort), an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.

Pancuronium dibromide (Pavulon), a competitive AChR antagonist (IC₅₀ = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide(Pancuronium bromide) blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.

Loteprednol etabonate (Lotemax) is an ophthalmic analog of the corticosteroid prednisolone with anti-inflammatory activity.

Cyproterone acetate (Cyproterone 17-O-acetate) binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.Cyproterone binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone Acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.

Mometasone furoate (Sch32088) is a pregnadienediol derivative with anti-allergic and anti-inflammatory properties, used in the management of asthma and allergic rhinitis, as well as a topical treatment for skin disorders.

Adrenosterone (11-ketoandrostenedione) is a steroid hormone isolated from the adrenal cortex.

Nandrolone phenylpropionate (Nandrolone phenpropionate) is an androgen receptor agonist. It mainly used to treat women with breast cancer and osteoporosis

11-Beta-hydroxyandrostenedione (NSC-17102) is a steroid mainly found in the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue), which is a 11β-hydroxysteroid dehydrogenase isozymes inhibitor. Measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism with 4-androstenedione increases.

Estrone sulfate sodium (17β-Estrone 3-sulfate) is an endogenous steroid and an estrogen ester that is biologically inactive. It is converted by steroid sulfatase into estrone . Estrone sulfate sodium has been investigated as a ligand for targeting organic anion transporting polypeptides f

1. Periplocin (Periplocoside) has anti-cancer effects on lung cancer cells, induces apoptosis and inhibits growth of cancer cells by the beta-catenin/Tcf signaling pathway. 2. Periplocin is used for treatment of rheumatoid arthritis, reinforcement of bones and tendons, palpitations or shortness of breath and lower extremity edema in traditional medicine.

Cerevisterol is a cytotoxic steroid, can inhibit the activity of DNA polymerase alpha. It can stimulate NGF-mediated neurite outgrowth on PC12 cells.

Ecdysone is a major steroid hormone in insects and herbs. Ecdysone triggers mineralocorticoid receptor activation and induces cellular apoptosis. Ecdysone signaling through Ecdysone receptor isoform B1 is required cell autonomously for the muscle death.

Steroid sulfatase-IN-9 (compound 54E) is a steroid sulfatase inhibitor with an inhibition rate of 87.03% at 10 μM. It shows no toxic effects on zebrafish larvae.

Steroid sulfatase-IN-10 (Example 216) is a potent inhibitor of steroid sulfatase, with an IC₅₀ range of 0.03-0.27 µM. It is applicable in research on inflammatory diseases such as rheumatoid arthritis, type 1 and type 2 diabetes, and systemic lupus erythematosus.

Steroid sulfatase-IN-11 is an inhibitor of the steroid sulfatase enzyme (Steroid Sulfatase), effectively reducing the enzyme's ability to hydrolyze steroid sulfates. It is applicable for research in hormone-dependent cancers.

Steroid sulfatase-IN-2 is an active inhibitor of steroid sulfatase (STS), demonstrating an IC₅₀ value of 109.5 nM. Its potential application lies in hormone-dependent cancer research, specifically estrogen-dependent breast and endometrial cancer [1].

Steroid sulfatase-IN-3 (compound 1q) is a potent STS inhibitor with an IC₅₀ value of 25.8 nM and exhibits antiproliferative effects against T-47D estrogen-dependent breast cancer cells, with an IC₅₀ of 1.04 μM [1].

Steroid sulfatase-IN-1 is a highly potent and orally active inhibitor of the enzyme Steroid sulfatase, with an impressive IC₅₀ value of 1.71 μM. This compound exhibits notable antitumor activity, achieving a TGI (tumor growth inhibition) of 51% in vivo, holding great promise in breast cancer research [1].

Steroid sulfatase/17β-HSD1-IN-1 is a highly effective inhibitor of steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities, with an IC₅₀ value of 28 nM against cellular human steroid sulfatase. This compound holds significant potential for investigating estrogen-dependent diseases [1].

Steroid sulfatase/17β-HSD1-IN-4 (compound 37) is a potent dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-4 irreversibly inhibits hSTS activity (IC₅₀= 63 nM) and has research value in endometriosis and other estrogen-dependent diseases.

Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 [17β-HSD1], useful in studying endometriosis and other estrogen-dependent diseases.

Steroid sulfatase-IN-4 (Compound 16) is an irreversible inhibitor of human steroid sulfatase (STS) with an IC₅₀ of 25 nM, and can be used to study endometriosis.

Steroid sulfatase-IN-7 is an irreversible inhibitor of steroid sulfatase (STS) with an IC₅₀ of 0.05 nM against human placental STS, making it suitable for cancer research applications [1].

Steroid Sulfatase-IN-6 (Compound 10c) serves as an irreversible steroid sulfatase (STS) inhibitor, exhibiting a K i value of 0.4 nM against human placenta STS, and is applicable in tumor disease research [1].