Calcitriol (Synonyms: 1,25-dihydroxy Cholecalciferol, 1α,25-dihydroxy Cholecalciferol, 1,25-dihydroxy Vitamin D3, 1α,25-dihydroxy Vitamin D3) |
Catalog No.GC13852
One-Click Copy Product Info
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Calcitriol is a hormonally active vitamin D analog with cellular penetration property.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 32222-06-3
Sample solution is provided at 25 µL, 10mM.
Calcitriol is a hormonally active vitamin D analog with cellular penetration property[1]. Calcitriol binds to vitamin D receptors in the kidneys, parathyroid glands, intestines, and bones to increase serum blood calcium levels by promoting absorption in the intestines, renal tubular reabsorption in the kidneys, and release from bone[2]. Calcitriol has been widely used in tumor research to regulate mitotic signaling and interfere with the proliferation of various cancer cells[3].
In vitro, Calcitriol treatment for 24 hours significantly suppressed the viability of BXPC-3, MCF-7 and PC-3 cells, with IC50 values of 21μM, 11.43μM and 9.53μM, respectively[4]. Treatment with 0.44μM Calcitriol for 24 hours induced apoptosis in B16-F10 cells, accompanied by an increase in the protein levels of cleaved caspase-3, caspase-8, caspase-9, Beclin and PARP[5]. Treatment with 10nM Calcitriol for 48 hours reduced the expression of COX-2 protein in LNCaP cells, increased the expression level of 15-PGDH protein, and restrained cell growth[6].
In vivo, Calcitriol treatment via topical application of dorsal skin at a dose of 1nmol (dissolved in 150μl ethanol) for 4 days markedly mitigated skin barrier dysfunction in atopic dermatitis NC/Nga mice, decreased epidermal thickness and the levels of IL-13 and IL-33[7]. Daily intraperitoneal injection of Calcitriol (5μg/kg) for 14 days alleviated the inflammatory cell infiltration in the lungs of mice induced by bleomycin (BLM) and inhibited the pulmonary epithelial-mesenchymal transition[8]. Intraperitoneal injection of Calcitriol at a dose of 5µg/kg every other day for 16 days reduced neuroinflammation, alleviated spinal cord inflammation, and attenuated demyelination in a mouse model of experimental autoimmune encephalomyelitis (EAE)[9].
References:
[1] Díaz L, Díaz-Muñoz M, García-Gaytán A C, et al. Mechanistic effects of calcitriol in cancer biology[J]. Nutrients, 2015, 7(6): 5020-5050.
[2] Trump D L, Hershberger P A, Bernardi R J, et al. Anti-tumor activity of calcitriol: pre-clinical and clinical studies[J]. The Journal of steroid biochemistry and molecular biology, 2004, 89: 519-526.
[3] Beer T M, Myrthue A. Calcitriol in cancer treatment: from the lab to the clinic[J]. Molecular Cancer Therapeutics, 2004, 3(3): 373-381.
[4] Kang Z S, Wang C, Han X L, et al. Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity[J]. European Journal of Medicinal Chemistry, 2018, 157: 1174-1191.
[5] Sutedja E K, Amarassaphira D, Goenawan H, et al. Calcitriol inhibits proliferation and potentially induces apoptosis in B16–F10 cells[J]. Medical science monitor basic research, 2022, 28: e935139-1.
[6] Moreno J, Krishnan A V, Swami S, et al. Regulation of prostaglandin metabolism by calcitriol attenuates growth stimulation in prostate cancer cells[J]. Cancer research, 2005, 65(17): 7917-7925.
[7] Umehara Y, Trujillo-Paez J V, Yue H, et al. Calcitriol, an active form of vitamin D3, mitigates skin barrier dysfunction in atopic dermatitis NC/Nga mice[J]. International Journal of Molecular Sciences, 2023, 24(11): 9347.
[8] Tan Z X, Chen Y H, Xu S, et al. Calcitriol inhibits bleomycin-induced early pulmonary inflammatory response and epithelial–mesenchymal transition in mice[J]. Toxicology letters, 2016, 240(1): 161-171.
[9] De Oliveira L R C, Mimura L A N, Fraga-Silva T F C, et al. Calcitriol prevents neuroinflammation and reduces blood-brain barrier disruption and local macrophage/microglia activation[J]. Frontiers in pharmacology, 2020, 11: 161.
| Cell experiment [1]: | |
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Cell lines |
B16-F10 cells |
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Preparation Method |
B16-F10 cells were cultured in DMEM medium, supplemented with 15% fetal bovine serum (FBS), 100U/ml penicillin and 100µg/ml streptomycin at 37°C in an incubator with 5% CO2. B16-F10 cells (1.7×102 cells/well) were seeded in a 96-well plate in a volume of 100μl. After 24h, cells were treated with various concentrations of Calcitriol (0, 0.02, 0.04, 0.08, 0.16, and 0.32μM) for 24h, cell viability was measured. |
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Reaction Conditions |
0, 0.02, 0.04, 0.08, 0.16, and 0.32μM; 24h |
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Applications |
Calcitriol treatment decreased cell viability of B16-F10 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6J mice |
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Preparation Method |
Female C57BL/6J mice (9 weeks old) were subcutaneously immunized at the base of the tail with 100μg of MOG35–55 emulsified with complete Freund's adjuvant (CFA) containing 4mg/ml of Mycobacterium tuberculosis. Mice received two intraperitoneal doses of Bordetella pertussis toxin at 200ng each: one at the immunization day and the other 48h after EAE induction. Body weight and disease scores were recorded daily. Disease clinical scores were defined according to the following manifestations: no symptoms (0); limp tail (1); hind leg weakness (2); partially paralyzed hind legs (3); complete hind leg paralysis (4); and complete paralysis (5). Intraperitoneal injection of Calcitriol at a dose of 5µg/kg every other day for 16 days was performed, and lumbar spinal cord samples were collected from mice for analysis. |
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Dosage form |
5µg/kg; every other day; 16 days; i.p. |
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Applications |
Calcitriol treatment attenuated inflammation and demyelination at the spinal cord in mice with EAE. |
References: [1] Sutedja E K, Amarassaphira D, Goenawan H, et al. Calcitriol inhibits proliferation and potentially induces apoptosis in B16–F10 cells[J]. Medical science monitor basic research, 2022, 28: e935139-1. [2] De Oliveira L R C, Mimura L A N, Fraga-Silva T F C, et al. Calcitriol prevents neuroinflammation and reduces blood-brain barrier disruption and local macrophage/microglia activation[J]. Frontiers in pharmacology, 2020, 11: 161. | |
| Cas No. | 32222-06-3 | SDF | |
| Synonyms | 1,25-dihydroxy Cholecalciferol, 1α,25-dihydroxy Cholecalciferol, 1,25-dihydroxy Vitamin D3, 1α,25-dihydroxy Vitamin D3 | ||
| Chemical Name | (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol | ||
| Canonical SMILES | CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C | ||
| Formula | C27H44O3 | M.Wt | 416.64 |
| Solubility | ≥ 20.832mg/mL in DMSO | Storage | -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use. |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Related Biological Data
VD reduces ferroptosis induced by high glucose in HK-2 cells and down-regulation of Klotho attenuates the protective effect of VD on ferroptosis in HK-2 cells. (F-K) Protein levels of SLC7A11, GPX4, TFR1, Klotho and p53 were detected by western blot.
HG + VD group (30 mmol/L D-glucose + 10 nmol/L 1,25(OH)2D3);1,25(OH)2D3 (GLPBIO, Beijing, China) was pretreated for 2 h before intervention.
Apoptosis (2024): 1-13. PMID: 38558206 IF: 7.2002 -
Related Biological Data
Effect of vitamin D deficiency on migration of human trophoblast cells. D&E: Cell migration was measured using wound-healing assay. After 12 and 24 h migration, the scratches were photographed and wounded areas were calculated.
And calcitriol (GLPBIO, China) was dissolved in DMSO at the final concentration of 1 mM, and the final concentration of calcitriol were 0.1 μM.
Placenta (2022). PMID: 36103800 IF: 3.2867
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