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.

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

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.

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.

Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.

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.

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.

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.

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

Formosanin C is a diosgenin saponin with multiple biological activities. Formosanin C possesses multiple anti-tumor mechanisms, including inducing apoptosis and autophagy, blocking the cell cycle, inhibiting metastasis and inducing ferroptosis. Formosanin C can inhibit the NF-κB signaling pathway to exert anti-inflammatory effects, and enhance the activity of immune cells. Formosanin C exhibits the inhibiting effect against C. albicans. Formosanin C can be used for the study of anti-inflammation, antifungal anti and anti-cancer (including lung cancer, liver cancer, breast cancer and colorectal cancer, etc.).

Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid X receptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases.

Maxacalcitol (22-Oxacalcitriol), a vitamin D3 (HY-15398) analog, is an orally active VDR agonist. Maxacalcitol has a limited calcemic effect. Maxacalcitol has the potential for psoriasis and hyperparathyroidism research.