Secosteroids

Calcipotriol is a synthetic VitD₃ analogue with a high affinity for the vitamin D receptor.

Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

25-Hydroxycholesterol (25-OHC) is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC₅₀≈65 nM) and selective suppressor of IgA production by B cells.

Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.

7-Ketocholesterol is an oxidation product of cholesterol, widely present in atherosclerotic plaques, and has a stronger atherogenic effect than cholesterol. 7-Ketocholesterol can inhibit the rate-limiting enzymes involved in bile acid and cholesterol synthesis, such as cholesterol 7α-hydroxylase and HMG-CoA reductase. 7-Ketocholesterol exhibits pro-inflammatory effects both in vivo and in vitro and can induce cell apoptosis (apoptosis).

Dioscin (CCRIS 4123; Collettiside III) is a natural plant-derived steroidal saponin that has good anti-cancer activity against a variety of cancer cells. Dioscin causes DNA damage and induces apoptosis in HeLa and SiHa cells. Dioscin regulates ROS-mediated DNA damage and mitochondrial signaling pathways, exerting anticancer activity.

Calcipotriol monohydrate is a synthetic VitD3 analogue with a high affinity for the vitamin D receptor.

Proscillaridin A is a potent poison of topoisomerase I/II activity with IC₅₀ values of 30 nM and 100 nM, respectively.

Calcifediol (25-hydroxy Vitamin D3) is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels.

Paricalcitol, a vitamin D analogue, is a vitamin D receptor agonist, used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.

Tachysterol 3 is a photoproduct of Previtamin D₃ (HY-130705). Previtamin D3 is an orally active, thermolabile steroidal compound that generates vitamin D3, as well as biologically inactive lumisterol and tachysterol. Previtamin D3 is synthesized in the skin of humans and rats via the UV-B-mediated photoconversion of 7-dehydrocholesterol. Previtamin D3 lacks direct anti-rachitic activity, and its in vivo activity relies on the vitamin D3 it produces. Previtamin D3 can be used in studies related to rickets and vitamin D metabolism.

Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D.

Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.

Eldecalcitol (ED-71) is an orally active vitamin D3 analogue, inhibits bone resorption and increases bone mineral density. Eldecalcitol (ED-71) displays anti-tumor effect and inhibits cell proliferation, migration and induces apoptosis by suppressing GPx-1.

Secalciferol ((24R)-24,25-Dihydroxyvitamin D3) is the major active metabolite of Vitamin D. Secalciferol activates vitamin D receptor (VDR) with an EC₅₀ value of 150 nM. Secalciferol is involved in a wide range of biological functions such as calcium homeostasis, cellular differentiation and proliferation processes, as well as other functions related to the immune system, which is promising for research of rickets, osteomalacia, hypercalcemia and autoimmune disorders.

Ercalcidiol is a metabolite of vitamin D₂, is regarded as an indicator of vitamin D nutritional status.

22 (R)-Hydroxycholesterol (Narthesterol) is a natural oxysterol, acting as a LXRα agonist that inhibits cancer cell proliferation. 22 (R)-Hydroxycholesterol activates LXRα-mediated upregulation of downstream ABCA1 expression, enhances apolipoprotein-dependent cholesterol efflux, reduces intracellular cholesterol content, and decreases the production of β-amyloid peptide. 22 (R)-Hydroxycholesterol induces the differentiation of human mesenchymal stem cells into functional dopaminergic neurons. 22 (R)-Hydroxycholesterol is applicable to research related to cancer, Alzheimer's disease, and Parkinson's disease.

ZK168281 is a 25-carboxylic ester 1α,25(OH)₂D₃ analog and a pure VDR antagonist with a K_d value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.

7β-Hydroxycholesterol is an oxysterol that derived by the oxidation of cholesterol. 7β-hydroxycholesterol can induce cellular oxidative stress, apoptosis, and necrosis, resulting in cytotoxicity. 7β-hydroxycholesterol has antitumor activity.

Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.