vdr

VDR agonist 1 (compound 28), a nonsteroidal Vitamin D receptor (VDR) agonist, demonstrates potent activity with a low IC 50 of 690 nM in MCF-7 cells. It inhibits cell cycle progression through upregulation of p21 and p27, and induces apoptosis by elevating BAX expression while reducing Bcl-2 levels [1].

ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist (Kd of 0.1 nM), efficiently inhibiting the coactivator (CoA) interaction with its receptor.

TEI-9647 is a 1α,25-dihydroxy vitamin D3-26,23-lactone (1α,25-lactone) analog and is an effective VDR/vitamin D-responsive element (DRE)-mediated genomic actions antagonist.

Inecalcitol is a unique vitamin D3 analog that induces apoptosis and has anticancer activity. It is an orally active vitamin D receptor agonist with a Kd of 0.53 nM.

Calcitriol (1,25-Dihydroxyvitamin D3) is a metabolite of vitamin D and a vitamin D receptor (VDR) agonist (IC50=0.4 nM). Calcitriol increases intestinal absorption of calcium and phosphorus, and increases bone resorption with parathyroid hormone.

Ergocalciferol (Vitamin D2 (Calciferol)) is a derivative of ergosterol formed by ultraviolet rays breaking of the C9-C10 bond with a strong inhibitory effect against bladder tumor promotion by sodium saccharin, and it induces cell differentiation in leukemia cells. Vitamin D2 is an inhibitor of DNA Polymerase.

Vitamin D3 (cholecalciferol) is a naturally occurring form of vitamin D; once metabolically activated, it can induce cellular differentiation and cancer cell proliferation. Vitamin D3 can be used to establish kidney stone models and is also an important research target in the fields of immunology and oncology.

25,26-Dihydroxyvitamin D3 (25,26-Dihydroxycholecalciferol) is a vitamin D3 metabolite and a precursor compound for the synthesis of 25-hydroxyvitamin D.

Calcipotriol (MC 903) is a synthetic vitamin D3 analogue with high affinity for the vitamin D receptor.

Maxacalcitol (22-Oxacalcitriol) is a ligand of VDR-like receptors and a non-serum calcium vitamin D3 analogue. Maxacalcitol inhibits parathyroid hormone (PTH) mRNA expression in vitro and in vivo.

Calcitriol Impurities D (24-Homo Calcitriol) is a hormonal form of the vitamin that promotes the differentiation of HL-60 human promyelocytic leukemia cells into monocytes.Calcitriol Impurities D has bone resorption activity and inhibits the replication of human immunodeficiency virus in human cells.Calcitriol Impurities D has antiviral activity and can be used to treat AIDS and viral infections. 25-dihydroxyvitamin D3 has antiviral activity and can be used in the treatment of AIDS and viral infections.

(24S)-24,25-Dihydroxyvitamin D3 undergoes multiple hydroxylation processes to form active vitamin D3 analogs.

Doxercalciferol (TSA 840) is a synthetic vitamin D2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.

Alfacalcidol (Etalpha) (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication.

Calcifediol (U 32070E) is a naturally occurring product that is metabolized in the liver from vitamin D3, a VDR ligand. Calcifediol is indicated for use as a vitamin supplement for all patients with vitamin D deficiency.

Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), the primary circulating metabolite of Vitamin D3, serves as a potent VDR inhibitor.

Paricalcitol is a selective vitamin D receptor agonist and a vitamin D analog. Paricalcitol potently inhibits the synthesis and secretion of parathyroid hormone (PTH) and is commonly used in studies of secondary hyperparathyroidism in patients with chronic kidney disease.

Calcipotriol monohydrate is an analog of Vitamin D3 with a high affinity for the vitamin D receptor. Calcipotriol monohydrate can be used for studies about psoriasis.

VDR agonist 3 (Compound E15) is a potent activator of the vitamin D receptor (VDR). It effectively inhibits the activation of hepatic stellate cells (HSC) via VDR. In a model of liver fibrosis induced by CCl4 in mice, VDR agonist 3 significantly alleviates liver fibrosis without causing hypercalcemia.

VDR agonist 4 is a potent VDR agonist that is effective when administered orally. It exhibits VDR-dependent antifibrotic activity by modulating various fibrosis-related genes, thereby inhibiting the production of α-SMA and collagen I and suppressing the activation of hepatic stellate cells. VDR agonist 4 can ameliorate liver fibrosis in mice induced by CCl4 and is useful for research related to liver fibrosis.

VDR ligand-1 (compound 13a) is a non-steroidal VDR agonist with an EC50 value of 16 nM. It is useful for research related to osteoporosis, psoriasis, and cancer.

VDR agonist 2 (compound 16i), a vitamin D receptor (VDR) agonist, effectively inhibits TGF-β1-induced hepatic stellate cell (HSC) activation, demonstrating notable anti-hepatic fibrosis efficacy both in vitro and in vivo [1].

MeTC7 is a vitamin D receptor (VDR) antagonist with antitumor activity that inhibits PD-L1 and may inhibit the growth of xenografts and transgenic tumors in vivo.

Triciferol acts as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR ( IC 50 =87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Triciferol also exhibits efficacious antiproliferative and cytotoxic activities in cancer cell models in vitro [1].