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Secalciferol

Catalog No.GC37614 Copy One-Click Copy Product Info

Secalciferol is a fat-soluble vitamin derived from plants and fungi, also known as (24R)-24,25-Dihydroxyvitamin D3. Secalciferol activates the vitamin D receptor (VDR) with an EC50 of 150nM.

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Secalciferol Chemical Structure

Cas No.: 55721-11-4

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1mg
$432.00
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Sample solution is provided at 25 µL, 10mM.



Description of Secalciferol

Secalciferol is a fat-soluble vitamin derived from plants and fungi, also known as (24R)-24,25-Dihydroxyvitamin D3. Secalciferol activates the vitamin D receptor (VDR) with an EC50 of 150nM[1-2]. Secalciferol is involved in various biological functions, including calcium homeostasis, cell differentiation, proliferation processes, and other functions related to the immune system. Secalciferol can be used in research on rickets, osteomalacia, hypercalcemia, and autoimmune diseases[3-4].

In vitro, Secalciferol (100pM - 10μM) was used to treat the IZ-VDRE and IZ-CYP24 stably transfected reporter gene cell lines for 24 hours. Secalciferol demonstrated a dose-dependent activation of the vitamin D receptor (VDR). The half-maximal effective concentration (EC50) of Secalciferol in the IZ-VDRE and IZ-CYP24 cell lines was 140.8nM and 166.1nM[5]. In the chondrogenic ATDC5 cell differentiation model, treatment with Secalciferol (0.1μM) for 7-14 days enhanced the gene expression of type 2 collagen (Col2a1) in Tlcd3b2-overexpressing cells, promoted proteoglycan synthesis, and facilitated the early differentiation of chondrocytes[6].

In vivo, Cyp24a1 knockout (Cyp24a1-/-) mice in a fracture repair model received subcutaneous injections of Secalciferol (6.7μg/kg/day) for 15 days. Secalciferol significantly corrected the defects in callus formation and callus stiffness during fracture repair in Cyp24a1-/- mice, restored callus volume, and improved the mechanical properties of the callus[7]. In hypophosphatemic (Hyp) mice, daily intraperitoneal injections of Secalciferol (1-1000μg/kg/day) for 28 days. Secalciferol significantly promoted bone formation in the lumbar vertebrae and improved bone formation parameters such as bone volume/tissue volume ratio and mineral apposition rate in a dose-dependent manner[8].

References:
[1] Henderson CM, Fink SL, Bassyouni H, et al. Vitamin D-Binding Protein Deficiency and Homozygous Deletion of the GC Gene. The New England Journal of Medicine. 2019 Mar;380(12):1150-1157.
[2] Wilson RT, Roff AN, Dai PJ, et al. Genetic Ancestry, Skin Reflectance and Pigmentation Genotypes in Association with Serum Vitamin D Metabolite Balance. Hormone Molecular Biology and Clinical Investigation. 2011 Sep;7(1):279-293.
[3] Makris K, Bhattoa HP, Cavalier E, et al. Recommendations on the measurement and the clinical use of vitamin D metabolites and vitamin D binding protein - A position paper from the IFCC Committee on bone metabolism. Clinica Chimica Acta; International Journal of Clinical Chemistry. 2021 Jun;517:171-197.
[4] Ikezaki S, Nishikawa A, Furukawa F, et al. Influences of long-term administration of 24R, 25-dihydroxyvitamin D3, a vitamin D3 derivative, in rats. J Toxicol Sci. 1999 May;24(2):133-9.
[5] Bartonkova I, Grycova A, Dvorak Z. Profiling of Vitamin D Metabolic Intermediates toward VDR Using Novel Stable Gene Reporter Cell Lines IZ-VDRE and IZ-CYP24. Chem Res Toxicol. 2016 Jul 18;29(7):1211-22.
[6] Antonyan L, Martineau C, St-Arnaud R. The ER protein TLC domain 3B2 and its enzymatic product lactosylceramide enhance chondrocyte maturation. Connect Tissue Res. 2021 Mar;62(2):176-182.
[7] Martineau C, Naja RP, Husseini A, et al. Optimal bone fracture repair requires 24R,25-dihydroxyvitamin D3 and its effector molecule FAM57B2. J Clin Invest. 2018 Aug 1;128(8):3546-3557.
[8] Ono T, Tanaka H, Yamate T, et al. 24R,25-dihydroxyvitamin D3 promotes bone formation without causing excessive resorption in hypophosphatemic mice. Endocrinology. 1996 Jun;137(6):2633-7.

Protocol of Secalciferol

Cell experiment [1]:

Cell lines

ATDC5 cells (mouse chondrogenic teratocarcinoma cell line)

Preparation Method

The ATDC5 prechondrogenic cells were cultured in DMEM/F12 medium supplemented with 5% FBS. For differentiation, ATDC5 cells were cultured in DMEM/F12 medium supplemented with Insulin-Transferrin-Sodium Selenite (ITS). Where indicated, cells were treated with Secalciferol (0.1μM) in charcoal-stripped FBS.

Reaction Conditions

0.1μM; 14 day.

Applications

In ATDC5 cells overexpressing Tlcd3b2, treatment with 0.1μM Secalciferol significantly increased the gene expression of the early chondrogenic differentiation marker Col2a1 compared to untreated cells.

Animal experiment [2]:

Animal models

Hypophosphatemic (Hyp) mice (a model for X-linked hypophosphatemic rickets) and normal control mice.

Preparation Method

The mice were divided into groups and received daily intraperitoneal injections for 28 days. Hyp mice received either Secalciferol at doses of 1-1000μg/kg/day. Control mice received no treatment or vehicle.

Dosage form

1-1000μg/kg/day; i.p.; Daily for 28 days.

Applications

Treatment of Hyp mice with Secalciferol dose-dependently promoted bone formation in the fifth lumbar (L5) vertebrae, as evidenced by increased parameters such as the length of the L5 spine, mineral apposition rate (MAR), and mineralized bone volume/bone volume (Md.BV/BV).

References:
[1] Antonyan L, Martineau C, St-Arnaud R. The ER protein TLC domain 3B2 and its enzymatic product lactosylceramide enhance chondrocyte maturation. Connect Tissue Res. 2021 Mar;62(2):176-182.
[2] Ono T, Tanaka H, Yamate T, et al. 24R,25-dihydroxyvitamin D3 promotes bone formation without causing excessive resorption in hypophosphatemic mice. Endocrinology. 1996 Jun;137(6):2633-7.

Chemical Properties of Secalciferol

Cas No. 55721-11-4 SDF
Canonical SMILES C=C(CC1)/C(C[C@H]1O)=C\C=C2[C@@]3([H])[C@@](CCC\2)(C)[C@@H]([C@H](C)CC[C@@H](O)C(C)(C)O)CC3
Formula C27H44O3 M.Wt 416.64
Solubility DMSO : 100 mg/mL (240.02 mM; Need ultrasonic); Ethanol : 50 mg/mL (120.01 mM; Need ultrasonic) Storage Store at -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use.
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Secalciferol

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.4002 mL 12.0008 mL 24.0015 mL
5 mM 480 μL 2.4002 mL 4.8003 mL
10 mM 240 μL 1.2001 mL 2.4002 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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