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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(24S)-24,25-Dihydroxyvitamin D3

(24S)-24,25-Dihydroxycholecalciferol is an inactive form of vitamin D3 which undergoes various levels of hydroxylation to form active vitamin D3 analogs. IC50 value:Target: Vitamin D3 analog1α-Hydroxyvitamin D3 (alfacalcidol) is a synthetic analog that is metabolized to 1,25-dihydroxycholecalciferol, the biologically active form of vitamin D3. Other analogues of cholecalciferol result from different hydroxylations. 24S,25-Dihydroxyvitamin D3 should not be confused with 24R,25-Dihydroxyvitamin D3.

  • CAS Number: 55700-58-8
  • MF: C27H44O3
  • MW: 416.63600
  • Catalog: VD/VDR
  • Density: 1.06g/cm3
  • Boiling Point: 571.1ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 241.5ºC

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

1alpha, 25-Dihydroxy VD2-D6

1alpha, 25-Dihydroxy VD2-D6 is a deuterated form of vitamin D.

  • CAS Number: 216244-04-1
  • MF: C28H38D6O3
  • MW: 434.68400
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tacalcitol

Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium.IC50 value:Target: Tacalcitol modulates immunological and inflammatory processes. Tacalcitol induces nerve growth factor production in epidermal keratinocytes.

  • CAS Number: 57333-96-7
  • 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

(24R)-MC 976

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

  • CAS Number: 112828-09-8
  • MF: C27H42O3
  • MW: 414.62100
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

Secalciferol-d6

Secalciferol-d6 ((24R)-24,25-Dihydroxyvitamin D3-d6) is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification[1][2].

  • CAS Number: 1440957-55-0
  • MF: C27H38D6O3
  • MW: 422.68
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

Paricalcitol

Paricalcitol is a vitamin D receptor agonist, used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.

  • CAS Number: 131918-61-1
  • MF: C27H44O3
  • MW: 416.637
  • Catalog: VD/VDR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 564.8±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 238.3±24.7 °C

Tacalcitol monohydrate

Tacalcitol monohydrate (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium.IC50 value:Target: Tacalcitol modulates immunological and inflammatory processes. Tacalcitol induces nerve growth factor production in epidermal keratinocytes.

  • CAS Number: 93129-94-3
  • MF: C27H46O4
  • MW: 434.652
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Impurity of Doxercalciferol

Impurity of Doxercalciferol is an impurity of doxercalciferol, which is a synthetic analog of ergocalciferol (vitamin D2), used as a drug for secondary hyperparathyroidism and metabolic bone disease, and it suppresses parathyroid synthesis and secretion.

  • CAS Number: 127516-23-8
  • MF: C28H44O2
  • MW: 412.64800
  • 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

25-Hydroxycalciferol

Ercalcidiol is a metabolite of vitamin D2, is regarded as an indicator of vitamin D nutritional status.

  • CAS Number: 21343-40-8
  • MF: C28H44O2
  • MW: 412.648
  • Catalog: VD/VDR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 542.3±38.0 °C at 760 mmHg
  • Melting Point: 45-51ºC
  • Flash Point: 225.9±21.4 °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

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

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

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

Calcipotriene

Calcipotriol is a synthetic VitD3 analogue with a high affinity for the vitamin D receptor.

  • CAS Number: 112965-21-6
  • 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: 166-168ºC
  • Flash Point: 250.6±24.7 °C

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

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

Calcitetrol

Calcitetrol(1α, 24, 25-Trihydroxy VD3) is the hormonally active form of vitamin D with three hydroxyl groups.IC50 value:Target: Calcitriol increases blood calcium levels ([Ca2+]) by promoting absorption of dietary calcium from the gastrointestinal tract and increasing renal tubular reabsorption of calcium, thus reducing the loss of calcium in the urine. Calcitriol also stimulates release of calcium from bone by its action on the specific type of bone cells referred to as osteoblasts, causing them to release RANKL, which in turn activates osteoclasts.

  • CAS Number: 72203-93-1
  • MF: C27H44O4
  • MW: 432.63600
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

25,26-Dihydroxyvitamin D3

25,26-Dihydroxyvitamin D3(25,26-dihydroxycholecalciferol) is a metabolite of vitamin D3 with intestinal calcium transport activity.IC50 value:Target: VD metaboliteThe biological activity of synthetic 24,25 and 25,26 diOHD3 was studied in vitamin D-deficient rats. The purpose of this study was to investigate the influence of small doses of both metabolites (0.125-0.250 mug) upon intestinal calcium transport and bone calcium mobilization. Both metabolites were able to increase calcium absorption in rats maintained on a calcium-deficient diet, but failed to do it in rats on a normal calcium diet. Bilateral nephrectomy suppressed this effect. The "bone calcium mobilization" of both derivatives was measured in vitamin D and calcium- or phosphorus-deprived rats after one intravenous dose. When serum calcium was initially low, 24,25 and 25,26 diOHD3 increased serum calcium moderately, but the increment was only significant with 24,25 diOHD3.

  • CAS Number: 29261-12-9
  • MF: C27H44O3
  • MW: 416.63600
  • Catalog: VD/VDR
  • Density: 1.06g/cm3
  • Boiling Point: 575.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 243.7ºC

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

Calcitriol

Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

  • CAS Number: 32222-06-3
  • 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: 119-1210C
  • Flash Point: 238.4±24.7 °C

Vitamin D3-d7

Vitamin D3-D7 (Cholecalciferol-D7) is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells[1][2].

  • CAS Number: 1627523-19-6
  • MF: C27H37D7O
  • MW: 391.681
  • Catalog: VD/VDR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 496.4±24.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 214.2±15.1 °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

Calcifediol

Calcifediol (monohydrate) is a major circulating metabolite of vitamin D3, acting as a competitive inhibitor with an apparent Ki of 3.9 μM, suppresses PTH secretion and mRNA (ED50=2 nM).

  • CAS Number: 63283-36-3
  • MF: C27H46O3
  • MW: 418.65
  • Catalog: VD/VDR
  • Density: N/A
  • Boiling Point: 529.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 221.4ºC

Vitamin D4

Vitamin D4 is the active analogue of Vitamin D.

  • CAS Number: 511-28-4
  • MF: C28H46O
  • MW: 398.66400
  • Catalog: VD/VDR
  • Density: 0.96 g/cm3
  • Boiling Point: 504.9ºC at 760 mmHg
  • Melting Point: 96-98ºC
  • Flash Point: 219.2ºC