adrenocortical

BC 11-38 is a potent, selective PDE biodepressant which is mainly effective against PDE11 (IC50 : 0.28 μM).

Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active, selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) with an EC50 of 9 nM.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Mitotane (NCI-C04933) is a derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.

Trilostane (Win 24540) is a synthetic androstane derivative with adrenocortical suppressive properties, reversibly inhibiting 3 beta-hydroxysteroid dehydrogenase delta [5-4] isomerase in the adrenal cortex.

Roridin A (Roridine A), a compound isolated from Verruca sp., showed nematicidal activity against Meloidogyne incognita.Roridin A is cytotoxic and has immunomodulatory activity.Roridin A has been used in the study of adrenocortical hyperplasia (CAH) and Cushing's disease (CD).

Perthane is the diethyl derivative of common pesticide DDD. It may cause adrenocortical atrophy in humans,and also prevent the formation of spontaneous mammary carcinoma.

Flumethasone pivalate (Locorten) has antipruritic, anti-inflammatory, and vasoconstrictive properties and can be used in studies about adrenocortical suppression, cutaneous atrophy, plasma transcortin binding, and telangiectasia.

Dexamethasone acetate monohydrate is an adrenocortical steroid. It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, asthma, severe allergies, chronic obstructive lung disease, brain swelling, croup, and antibiotics

Eprosartan (SKF-108566J free base) is a selective, competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes, used as an antihypertensive agent. It exhibits inhibitory effects on angiotensin II receptors with IC50 values of 9.2 nM in rat adrenocortical membranes and 3.9 nM in human adrenocortical membranes.

Deoxycorticosterone acetate (Cortexone acetate) is the 21-acetate derivative of desoxycorticosterone, used for intramuscular injection for replacement therapy of the adrenocortical steroid.

Adrenomedullin (22-52) is a C-terminal fragment of adrenomedullin (1-52) . In vitro, adrenomedullin (22-52) reduces basal corticosterone production in a mixture of rat adrenocortical and adrenomedulllary cells. It also reverses increases in ACTH-stimulated corticosterone production induced by adrenomedullin (1-52). Adrenomedulin (22-52) (0.5 and 5 μg/kg/min) has no effect on basal regional cerebral blood flow but reverses increases in regional cerebral blood flow induced by rat adrenomedullin in rats. Unlike adrenomedullin (1-52), adrenomedullin (22-52) has no effect on mesenteric arterial perfusion pressure in cats.

Tetrahydro-11-deoxy cortisol (THS) is the primary urinary metabolite of 11-deoxycortisol. Urinary excretion of THS is elevated in patients with 11β-hydroxylase deficiency, a condition resulting from mutations in the cytochrome P450 (CYP) isoform CYP11B1. Urinary levels of THS are also elevated in patients with adrenocortical carcinoma (ACC) and adrenocortical adenoma (ACA) but are higher in patients with ACC compared to ACA.

Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) with IC50 values ​​of 2.5 and 0.7 nM, respectively, and has been approved by the FDA for the treatment of Cushing's disease.

Efonidipine HCl (NZ-105) serves as both a T-type and L-type calcium channel blocker. This compound, distinct from other calcium channel blockers, notably increases N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP)-induced StAR mRNA and DHEA-S production in NCI-H295R adrenocortical carcinoma cells, actions reflective of adrenocorticotropic hormone. Efonidipine uniquely inhibits calcium channels by merging tonic and use-dependent blocking methods. Its inhibitory concentrations (IC50) for I(Ca(T)) and I(Ca(L)) are 0.35 micromol l and 1.8 nmol l, respectively. Clinically, efonidipine administered to hypertensive patients undergoing chronic hemodialysis (20-60 mg, twice daily) demonstrated comparable blood pressure control to amlodipine (2.5-7.5 mg, once daily) over a 12-week period without significantly altering pulse rate. Furthermore, efonidipine significantly improved left ventricular ejection fraction in heart failure models without affecting blood pressure, in addition to lowering the heart rate by about 10%.

FHD-609, an inhibitor and degrader of BRD9 (bromodomain-containing protein 9), targets the ncBAF complex and is useful for researching a broad spectrum of cancers with mutations in a BAF complex subunit. When used alongside Telomelysin or INO5401, FHD-609 could be effective in treating adrenocortical carcinoma (ACC) [1] [2].

Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a Ca(2+)-channel blocker that enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells.

Atumelnant (CRN04894) is a selective and potent MC2R antagonist that inhibits ACTH-stimulated corticosterone secretion in a dose-dependent manner for the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).

CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) with MMAE, targeting folate receptor (FRα) and TRPV6. It exhibits high binding affinity to FRα and low affinity to TRPV6. CBP-1008 shows antitumor activity and can be utilized for research in advanced solid tumors such as colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.