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 that, after metabolic activation, can induce cell differentiation and cancer cell proliferation. It can also be used to establish kidney stone models.

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 vitamin D receptor agonist. It is used for the prevention and treatment of secondary hyperparathyroidism associated with chronic renal failure.

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 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].

24R-Calcipotriol (PRI 2202) is an impurity of Calcipotriol, a ligand of VDR-like receptors.

Alfacalcidol-D6 is a deuterated Alfacalcidol. Alfacalcidol is a non-selective VDR activator medication.