Date published: 2025-12-7

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VDR Activators

Vitamin D Receptor (VDR) activators are a class of chemical compounds that interact with the vitamin D receptor, a member of the nuclear receptor family of transcription factors. This receptor is primarily known for its role in calcium homeostasis and bone metabolism. VDR activators commonly function by binding to the ligand-binding domain of the receptor, which results in a conformational change that allows for the interaction with retinoid X receptors (RXRs). This heterodimer then binds to specific DNA sequences known as vitamin D response elements (VDREs), initiating the transcription of target genes. The specificity of this action is highly regulated and dependent on the presence of coactivators and corepressors, which modulate the transcriptional activity of the VDR. Some VDR activators like calcitriol are naturally occurring forms of vitamin D, while others like lithocholic acid are bile acids with the ability to bind to VDR. The mechanisms by which VDR activators modulate receptor expression can be diverse. Many of these compounds not only directly interact with VDR but also influence its expression or stability through various cellular pathways. For instance, some polyphenols can upregulate VDR expression through their anti-inflammatory effects, while certain fatty acids enhance VDR transcription via peroxisome proliferator-activated receptors (PPARs). Furthermore, compounds like resveratrol and curcumin affect VDR through pathways like SIRT1 activation and antioxidant activity, respectively. This multifaceted impact on VDR makes these compounds of particular interest in understanding the intricate biochemical networks within the cell.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

1α,25-Dihydroxyvitamin D3

32222-06-3sc-202877B
sc-202877A
sc-202877C
sc-202877D
sc-202877
50 µg
1 mg
5 mg
10 mg
100 µg
$325.00
$632.00
$1428.00
$2450.00
$400.00
32
(2)

Binds directly to VDR, promoting its activation

EB 1089

134404-52-7sc-358831A
sc-358831
sc-358831B
500 µg
1 mg
5 mg
$158.00
$208.00
$923.00
4
(1)

EB 1089 (CAS 134404-52-7) is a synthetic analog of calcitriol designed to activate the Vitamin D Receptor (VDR). It binds to VDR, inducing a structural shift that allows the receptor to form a heterodimer with retinoid X receptors (RXRs). This complex then engages with vitamin D response elements (VDREs) in DNA, initiating transcription of specific genes. Known for its high affinity for VDR, EB 1089 is commonly used in research to study VDR activation's biochemical and cellular impacts.

25-Hydroxyvitamin D3

19356-17-3sc-288574A
sc-288574
sc-288574B
sc-288574C
sc-288574D
sc-288574E
1 mg
5 mg
25 mg
500 mg
1 g
10 g
$106.00
$365.00
$773.00
$1324.00
$2266.00
$11830.00
13
(1)

25-Hydroxyvitamin D3 (CAS 19356-17-3) is a vitamin D3 metabolite that acts as a precursor to calcitriol, the active form with higher VDR affinity. It binds to VDR, undergoes a structural change, and forms a heterodimer with RXRs. This complex engages with VDREs in DNA to initiate gene transcription. It's a key compound for studying VDR activation.

Cholecalciferol

67-97-0sc-205630
sc-205630A
sc-205630B
1 g
5 g
10 g
$70.00
$160.00
$290.00
2
(1)

Cholecalciferol (CAS 67-97-0), also known as Vitamin D3, is a prohormone that serves as a precursor to the active form, calcitriol. It undergoes hydroxylation in the liver and kidneys to become an effective VDR activator. Once converted, it binds to VDR, triggering a conformational change that enables the receptor to form a heterodimer with retinoid X receptors (RXRs). This complex interacts with vitamin D response elements (VDREs) in DNA, initiating transcription of specific genes.

Ercalcitriol-d6

216244-04-1sc-353279
1 mg
$2352.00
(0)

Ercalcitriol-d6 (CAS 216244-04-1) is a deuterated form of ercalcitriol, which itself is an analog of calcitriol. It effectively activates the Vitamin D Receptor (VDR) by binding to it. This binding leads to a structural alteration in VDR, allowing it to heterodimerize with retinoid X receptors (RXRs). The resulting complex interacts with vitamin D response elements (VDREs) in DNA, initiating the transcription of specific genes involved in various cellular processes.

Vitamin D2, 1a-Hydroxy-

54573-75-0sc-205886
1 mg
$60.00
(1)

1α-Hydroxyvitamin D2 (CAS 54573-75-0) is a synthetic analog of the naturally occurring vitamin D2. It activates the Vitamin D Receptor (VDR) by binding directly to it. This interaction induces a conformational change in the VDR, enabling it to form a heterodimer with retinoid X receptors (RXRs). The resulting complex targets vitamin D response elements (VDREs) within DNA, initiating the transcription of specific genes crucial for cellular processes like calcium homeostasis.

Alfacalcidol-d7

sc-217598
10 mg
$19700.00
(0)

Alfacalcidol-d7 is a deuterated variant of alfacalcidol, a prodrug that is metabolized to calcitriol, the active form that binds to the Vitamin D Receptor (VDR). Upon binding, the VDR undergoes a conformational shift that allows it to heterodimerize with retinoid X receptors (RXRs). This complex interacts with vitamin D response elements (VDREs) in the DNA, initiating the transcription of target genes involved in various cellular activities such as calcium regulation.