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].

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].

Inecalcitol (TX 522) is the growth inhibitor of human breast cancer cells. Inecalcitol is a unique vitamin D3 analog with Kd of 0.53 nM.

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].

Calcifediol (U 32070E)(Ki of 3.9 μM), a major circulating metabolite of vitamin D3, works as a competitive inhibitor. It (ED50=2 nM)also inhibits PTH secretion and mRNA.

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.

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.

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

LG190178, a vitamin D receptor (VDR) ligand, is a therapeutic agent used for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism.

(1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3), a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3), exerts potent actions through vitamin D receptor (VDR) activation, including the inhibition of keratinocyte growth and suppression of parathyroid hormone secretion[1].

Impurity B of Calcitriol is an impurity of Calcitriol. Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).

TEI-9648, an analogue of Vitamin D3 Lactone, acts as a potent and specific antagonist to the vitamin D receptor (VDR). This compound effectively blocks the genomic actions mediated by VDR and the Vitamin D responsive element (VDRE) of 1α,25(OH)2D3. Furthermore, TEI-9648 prevents the differentiation of HL-60 cells induced by 1α,25(OH)2D3, indicating its utility in bone metabolism studies[1][2].

LG190155 is a moderately potent VDR agonist. Vitamin D receptor (VDR) agonists are well known for their capacity to control calcium and bone metabolism and to regulate growth and differentiation of many cell types.

ZK159222 is an effective 1α,25-(OH)2D3 receptor (VDR) agonist. ZK159222 has a partial agonistic character.

Maxacalcitol-D6 is a non-calcemic vitamin D3 analog and VDR ligand of VDR-like receptors.Maxacalcitol-D6 is the deuterated form of Maxacalcitol (22-Oxacalcitriol).

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

Calcipotriol (MC 903) is a synthetic VitD3 analogue. Which has a high affinity for the vitamin D receptor.

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

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.

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

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.

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

MeTC7 is a VDR antagonist, which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo.

MC 1046 is an impurity of Calcipotriol. Calcipotriol is a ligand of VDR-like receptors.

Impurity of Alfacalcidol is an impurity of Alfacalcidol. Alfacalcidol is a non-selective VDR activator medication.

Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), the main circulating metabolite of vitamin D3, is a potent VDR inhibitor.

Calcipotriol Impurity C is the impurity of Calcipotriol. Calcipotriol is a VDR-like receptors ligand.

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

PS121912 is a potent and selective inhibitor of VDR-coactivator.

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.

Impurity F of Calcipotriol is a impurity of Calcipotriol. Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.

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) , a naturally occurring form of vitamin D, activates an H305F/H397Y mutant vitamin D receptor (VDR).