Vitamin D was first identified as a cure for nutritional rickets, a disease of bone growth caused by an inadequate uptake of dietary calcium. Vitamin D refers collectively to vitamin D3 and vitamin D2. Biologically active vitamin D is generated via largely hepatic 25-hydroxylation catalyzed by CYP2R1, CYP27A1, and possibly other enzymes to produce 25-hydroxvitamin D (25D), which has a long half-life and is the major circulating vitamin D metabolite. 25D is modified by 1α-hydroxylation catalyzed by CYP27B1, which produces hormonal 1,25-dihydroxyvitamin D (1,25D).

The biological actions of 1,25(OH)2D3 are mediated by the VDR. VDR belongs to the steroid receptor family which includes receptors for retinoic acid, thyroid hormone, sex hormones, and adrenal steroids. The genomic mechanism of 1,25(OH)2D3 action involves the direct binding of the 1,25(OH)2D3 activated vitamin D receptor/retinoic X receptor (VDR/RXR) heterodimeric complex to specific DNA sequences. 1,25(OH)2D3 action regulates renal calcium reabsorption and phosphate loss, and thus control bone metabolism mainly indirectly by regulating mineral homeostasis.

Vitamin D deficiency increases rates of cancer, as well as autoimmune and infectious diseases. More than 3,000 vitamin D analogs are developed worldwide and several analogs demonstrated more potent antiproliferative and prodifferentating effects on cancer cell lines compared with 1,25(OH)2D3, which may lead to the development of new therapies to prevent and treat diseases.

References:
[1] White JH. Infect Immun. 2008 Sep;76(9):3837-43.
[2] Christakos S, et al. Physiol Rev. 2016 Jan;96(1):365-408.


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VD/VDR
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Alfacalcidol-D6

Alfacalcidol-D6, a deuterated Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3), is a non-selective VDR activator medication. IC50 value: Target: VDR activatorAlfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) improves mechanical bone strength and bone mass; suppresses osteoclastic bone resorption in vivo.

  • CAS Number: 1641940-94-4
  • MF: C27H38D6O2
  • MW: 406.674
  • Catalog: VD/VDR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 531.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.6±24.7 °C

CB1151

CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM[1].

  • CAS Number: 182369-28-4
  • MF: C28H46O4
  • MW: 446.66
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Seocalcitol

Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.

  • CAS Number: 134404-52-7
  • MF: C30H46O3
  • MW: 454.684
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 608.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 252.3±26.1 °C

Falecalcitriol

Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.

  • CAS Number: 83805-11-2
  • MF: C27H38F6O3
  • MW: 524.579
  • Catalog: VD/VDR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 576.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 302.7±30.1 °C

24 25-Dihydroxy VD3

24, 25-Dihydroxy VD3 is a compound which is closely related to 1,25-dihydroxyvitamin D3, the active form of vitamin D3, but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo.

  • CAS Number: 40013-87-4
  • MF: C27H44O3
  • MW: 416.63600
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VD3-D6

VD3-D6(Vitamin D3-26,26,26,27,27,27-d6) is the deuterated form of Vitamin D3; tools for determination of Vitamin D3 metabolites in human serum.

  • CAS Number: 118584-54-6
  • MF: C27H38D6O
  • MW: 390.67500
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VD2-D3

VD2-D3 is a deuterated form of vitamin D.

  • CAS Number: 1217448-46-8
  • MF: C28H41D3O
  • MW: 399.66700
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: 14 °C

Alfacalcidol

Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication. IC50 value: Target: VDR activatorAlfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) improves mechanical bone strength and bone mass; suppresses osteoclastic bone resorption in vivo.

  • CAS Number: 41294-56-8
  • MF: C27H44O2
  • MW: 400.637
  • Catalog: VD/VDR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 531.5±50.0 °C at 760 mmHg
  • Melting Point: 134-136°C
  • Flash Point: 222.6±24.7 °C

MeTC7

MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects[1].

  • CAS Number: 1817841-22-7
  • MF: C32H48BrN3O4
  • MW: 618.65
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vitamin D3

Cholecalciferol(Vitamin D3) is a naturally occuring form of vitamin D; Reported that upon metabolic activation, Cholecalciferol induces cell differentiation and prevents proliferation of cancer cells. IC50 value:Target: Vitamin D acts through a receptor that is a member of the ligand-dependent transcription factor superfamily. Modulates the proliferation and differentiation of both normal and cancer cells. Has antiproliferative and antimetastatic effects on breast, colon, and prostate cancer cells. Activated vitamin D receptors in intestine and bone maintain calcium absorbance and homeostasis.

  • CAS Number: 67-97-0
  • MF: C27H44O
  • MW: 384.638
  • Catalog: VD/VDR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 496.4±24.0 °C at 760 mmHg
  • Melting Point: 83-86 °C(lit.)
  • Flash Point: 214.2±15.1 °C

24-homo-1,25-dihydroxyvitamin D3

Calcitriol Impurities D is the 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).Target: vitamin D receptor

  • CAS Number: 103656-40-2
  • MF: C28H46O3
  • MW: 430.66300
  • Catalog: VD/VDR
  • Density: 1.055g/cm3
  • Boiling Point: 575.634°C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 240.469°C

HSDB 3314

Dihydrotachysterol is a synthetic analog of vitamin D. Dihydrotachysterol can be used to for the research of hypocalcemia (lack of calcium in the blood) and hypoparathyroidism (lack of parathyroid hormone in the body) [1][2].

  • CAS Number: 67-96-9
  • MF: C28H46O
  • MW: 398.66400
  • Catalog: VD/VDR
  • Density: 1.003 g/cm3
  • Boiling Point: 499.5ºC at 760 mmHg
  • Melting Point: 131ºC
  • Flash Point: 217.6ºC

vitamin D3-d3

Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.

  • CAS Number: 80666-48-4
  • MF: C27H41D3O
  • MW: 387.65600
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

11,12-Dihydroxyabieta-8(14),9(11),12-trien-7-one

11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR)[1].

  • CAS Number: 88664-08-8
  • MF: C20H28O3
  • MW: 316.43
  • Catalog: RAR/RXR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 482.2±45.0 °C at 760 mmHg
  • Melting Point: 192-194 °C
  • Flash Point: 259.5±25.2 °C

Calcitriol-d3

Calcitriol-d3 is the deuterium labeled Calcitriol[1]. Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist[2][3][4][5].

  • CAS Number: 128723-16-0
  • MF: C27H41D3O3
  • MW: 419.65500
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Maxacalcitol

Maxacalcitol (22-Oxacalcitriol) is non-calcemic vitamin D3 analog and ligand of VDR-like receptors. IC50 value:Target: Maxacalcitol (22-Oxacalcitriol)suppresses parathyroid hormone (PTH) mRNA expression in vitro and in vivo. Maxacalcitol exhibits similar effects to calcitriol in osteoblast-like cells. Maxacalcitol(22-Oxacalcitriol) inhibits tumor growth of osteosarcoma in vitro in combination with all-trans retinoic acid.

  • CAS Number: 103909-75-7
  • MF: C26H42O4
  • MW: 418.609
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 581.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 305.4±30.1 °C

3-O-(2-Aminoethyl)-25-hydroxyvitamin D3

3-O-(2-Aminoethyl)-25-hydroxyvitamin D3 is a Vitamin D3 derivative.

  • CAS Number: 163018-26-6
  • MF: C30H51NO2
  • MW: 457.73100
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5,6-trans-Calcitriol

Calcitriol Impurities A is the 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).Target: vitamin D receptor

  • CAS Number: 73837-24-8
  • MF: C27H44O3
  • MW: 416.637
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 565.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 238.4±24.7 °C

ZK159222

ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) agonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character[1].

  • CAS Number: 156965-15-0
  • MF: C32H48O5
  • MW: 512.721
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 646.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 201.1±25.0 °C

Eldecalcitol

Eldecalcitol (ED-71; 2.beta.-(3-Hydroxypropoxy)-1.alpha.,25-dihydroxyvitamin D3) is an analog of 1,25-dihydroxyvitamin D3 that improves bone mineral density. IC50 value:Target: Vd analogEldecalcitol (ED-71; 2.beta.-(3-Hydroxypropoxy)-1.alpha.,25-dihydroxyvitamin D3) is more efficacious than alfacalcidol in preventing vertebral and wrist fractures in osteoporotic patients with vitamin D sufficiency, with a safety profile similar to alfacalcidol.

  • CAS Number: 104121-92-8
  • MF: C30H50O5
  • MW: 490.715
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 655.7±55.0 °C at 760 mmHg
  • Melting Point: 126-128ºC
  • Flash Point: 350.3±31.5 °C

TEI-9647

TEI-9647 is a first and potent VDR/vitamin D-responsive element (DRE)-mediated genomic actions antagonist. TEI-9647 is a 1α,25-dihydroxyvitamin D3-26,23-lactone (1α,25-lactone) analogue[1].

  • CAS Number: 173388-20-0
  • MF: C27H38O4
  • MW: 426.58800
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: 618.492ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 204.543ºC

TEI-9648

TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research[1][2].

  • CAS Number: 173388-21-1
  • MF: C27H38O4
  • MW: 426.58800
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: 618.492ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 204.543ºC

MC 1046

MC 1046(Impurity A of Calcipotriol) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors. IC50 value:Target: Vitamin D3 analog that displays minimal effects on calcium homeostasis. Regulates cell differentiation and proliferation; Calcipotriol (MC 903; Calcipotriene) exhibits antiproliferative activity against human HL-60, HL60/MX2, MCF-7, T47D, SCC-25 and mouse WEHI-3 cancer cell lines.

  • CAS Number: 126860-83-1
  • MF: C27H38O3
  • MW: 410.589
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 584.2±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 321.1±26.6 °C

22-hydroxycholecalciferol

22-Hydroxyvitamin D3 a novel vitamin D analog, that displays no vitamin D agonist activity in the intestine or in bone[1].

  • CAS Number: 110927-46-3
  • MF: C27H44O2
  • MW: 400.63700
  • Catalog: VD/VDR
  • Density: 1.01g/cm3
  • Boiling Point: 529.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 221.4ºC

5,6-trans-Vitamin D3

5,6-trans-Vitamin D3 (5,6-trans-Cholecalciferol;5,6-trans-Colecalciferol) is a photoproduct of vitamin D3[1]. Vitamin D3 is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.

  • CAS Number: 22350-41-0
  • MF: C27H44O
  • MW: 384.63800
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Calcipotriol Impurity C

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

  • CAS Number: 113082-99-8
  • MF: C27H40O3
  • MW: 412.605
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 582.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 250.6±24.7 °C

(24S)-MC 976

(24S)-MC 976 is a Vitamin D3 derivative.

  • CAS Number: 112849-14-6
  • MF: C27H42O3
  • MW: 414.62100
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

24, 25-Dihydroxy VD2

24, 25-Dihydroxy VD2 is a hydroxylated metabolite of Vitamin D2; a synthetic analog of Vitamin D.

  • CAS Number: 58050-55-8
  • MF: C28H44O3
  • MW: 428.64700
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

24R-Calcipotriol

24R-Calcipotriol(PRI 2202) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.IC50 value:Target: Vitamin D3 analog that displays minimal effects on calcium homeostasis. Regulates cell differentiation and proliferation; Calcipotriol (MC 903; Calcipotriene) exhibits antiproliferative activity against human HL-60, HL60/MX2, MCF-7, T47D, SCC-25 and mouse WEHI-3 cancer cell lines.

  • CAS Number: 112827-99-3
  • MF: C27H40O3
  • MW: 412.60500
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZK168281

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

  • CAS Number: 186371-96-0
  • MF: C32H46O5
  • MW: 510.70500
  • Catalog: VD/VDR
  • Density: 1.151g/cm3
  • Boiling Point: 652.937ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 204.377ºC