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Chemical Structure| 32222-06-3 Chemical Structure| 32222-06-3

Structure of Calcitriol
CAS No.: 32222-06-3

Chemical Structure| 32222-06-3

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Calcitriol is the active form of Vitamin D3 with high affinity for the Vitamin D receptor (VDR), with an IC50 value of 1 nM. Calcitriol regulates calcium and phosphate metabolism, has anti-inflammatory and antitumor effects, and can be used in research on osteoporosis, chronic kidney disease, and cancer.

Synonyms: 1,25-Dihydroxyvitamin D3; 1α,25-dihydroxy Vitamin D3; 1,25(OH)2D

4.5 *For Research Use Only !

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Product Details of Calcitriol

CAS No. :32222-06-3
Formula : C27H44O3
M.W : 416.64
SMILES Code : C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCCC(C)(O)C)([H])/C(CCC1)=C/C=C3C([C@H](C[C@@H](C\3)O)O)=C
Synonyms :
1,25-Dihydroxyvitamin D3; 1α,25-dihydroxy Vitamin D3; 1,25(OH)2D
MDL No. :MFCD00867079

Safety of Calcitriol

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H300+H310+H330-H361
Precautionary Statements:P260-P262-P280-P301+P310+P330-P302+P352+P310-P304+P340+P310-P403+P233
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary cortical neurons 1 nM, 10 nM, 100 nM, 500 nM 24 h To evaluate the effect of Calcitriol on neuronal cell viability. The results showed that 1 nM and 10 nM Calcitriol had no toxic effect, while 100 nM and 500 nM Calcitriol significantly reduced cell viability. PMC8461874
AC16 cells 10 nM 24 h To study the effect of Calcitriol on TNF-α-induced AC16 cell death, results showed that Calcitriol significantly increased cell viability. PMC9139780
AC16 cells 100 nM 24 h To study the effect of Calcitriol on TNF-α-induced AC16 cell death, results showed that high-dose Calcitriol significantly increased cell viability. PMC9139780
SW480 cells 100 nM Calcitriol inhibited the proliferation and migration capacity of SW480 cells PMC8635240
LoVo cells 100 nM Calcitriol inhibited the proliferation and migration capacity of LoVo cells PMC8635240
FHC cells 100 nM Calcitriol promoted the proliferation of FHC cells PMC8635240
HL-1 atrial myocytes 1 nM and 10 nM 48 h To investigate whether Calcitriol downregulates FGFR1 expression through histone deacetylase (HDAC) activation. Results showed that Calcitriol significantly reduced FGFR1 expression in HL-1 cells. PMC5960138
osteoclast 1 nM, 10 nM, 100 nM overnight Calcitriol inhibited the fusion ability and the number of TRAP-positive differentiated osteoclasts in a dose-dependent manner. PMC6164019
preosteoblast 7F2 cells 1 nM, 10 nM, 100 nM overnight Calcitriol had no significant effect on Wnt 10b and Wnt 16 expression in preosteoblast 7F2 cells. PMC6164019

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
CD1 Elite mice Traumatic brain injury (TBI) model Gavage 0.5 µg/kg, 1 µg/kg, 3 µg/kg Once daily for 14 days To evaluate the neuroprotective effects of Calcitriol in TBI mice. The results showed that Calcitriol significantly ameliorated neurological deficits and histopathological changes following TBI, promoted the autophagic process, and activated Nrf2 signaling, thereby mitigating TBI-induced oxidative damage. PMC8461874
C57BL/6 mice 4-nitroquinoline-1-oxide (4NQO) induced oral carcinogenesis model Intraperitoneal injection 0.1 μg Monday, Wednesday, and Friday for 16 weeks, 10 weeks, or 26 weeks To evaluate the impact of Calcitriol on oral carcinogenesis at different stages of intervention and durations of exposure. Results showed that Calcitriol administered concurrently with 4NQO for 16 weeks significantly reduced premalignant lesions by 57%, while 26 weeks of Calcitriol treatment showed the highest renal CYP24A1 expression and the highest incidence of invasive SCC. PMC6416727
Kunming mice Myocardial infarction model Oral gavage 0.0375 µg/kg, 0.075 µg/kg, 0.15 µg/kg Once daily for 4 weeks To study the effect of Calcitriol on cardiac function and remodeling in MI mice, results showed that Calcitriol significantly improved cardiac function and reversed adverse cardiac remodeling. PMC9139780
nude mice SW480 cell-derived xenograft model intraperitoneal injection 50 μg/kg three times a week for 2 weeks Calcitriol significantly inhibited the growth of SW480 cell-derived xenograft tumors PMC8635240
C57BL/6J mice 5/6 nephrectomy CKD model oral gavage 25 IU/kg, 150 IU/kg daily for one month Calcitriol significantly promoted the growth of both trabecular and cortical bone in CKD mice, especially at the 150 IU/kg dose. PMC6164019

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03748966 X-linked Hypophosphatemia|Hypo... More >>phosphatemic Rickets|Hypophosphatemic Rickets, X-Linked Dominant Less << EARLY_PHASE1 RECRUITING 2025-03-25 Massachusetts General Hospital... More >>, Boston, Massachusetts, 02114, United States Less <<
NCT01120119 Diabetes Mellitus, Type 1 PHASE2 COMPLETED - University Campus Bio Medico, ... More >>Rome, 00128, Italy|Bambino Gesù Children's Hospital, Rome, Italy|Catholic University,, Rome, Italy|Sandro Pertini Hospital, Rome, Italy|University Sapienza, Rome, Italy Less <<
NCT01237028 IgA Nephropathy COMPLETED 2025-08-16 National Health Insurance Corp... More >>oration Ilsan Hospital, Goyang, 41-0719, Korea, Republic of|Kwandong University Myongji Hospital, Goyang, 412-270, Korea, Republic of|Wongkwang University Sanbon Medical Center, Gunpo, 435-040, Korea, Republic of|CHA University Bundang Medical Center, Seongnam, 435-040, Korea, Republic of|Seoul National University Hospital, Seoul, 110-752, Korea, Republic of|Severance Hospital, Seoul, 120-752, Korea, Republic of|Ewha Womans University Medical Center, Seoul, 158-710, Korea, Republic of Less <<
NCT00319761 IGA Nephropathy PHASE4 COMPLETED 2025-09-07 Department of Medicine & Thera... More >>peutics, Prince of Wales Hospital, Hong Kong, Hong Kong Less <<
NCT02125279 Psoriasis Vulgaris PHASE4 COMPLETED 2025-05-18 Johnson Dermatology, Fort Smit... More >>h, Arkansas, 72916, United States|Northwest Arkansas Clinical Trials Center, PLLC, Rogers, Arkansas, 72758, United States|Advanced Skincare Surgery & Medcenter, Burbank, California, 91505, United States|University of South Florida, Tampa, Florida, 33612, United States|Shideler Clinical Research Center, Carmel, Indiana, 46032, United States|Dawes Fretzin Clinical Research Group, Indianapolis, Indiana, 46256, United States|Montefiore Medical Center, New York, New York, 10467, United States|Arlington Research Center for Dermatology, Arlington, Texas, 76011, United States|UZ Gent Dermatology Department, Gent, 9000, Belgium|Lynderm Research Inc., Markham, Ontario, L3P1X2, Canada|CHU Sainte-Justine, Montreal, Quebec, H3T1C5, Canada|Charité Universit?tsmedizin Berlin, Berlin, 10117, Germany|University Hospital Carl Gustav Carus, Dresden, 01307, Germany|Universit?ts-Hautklinik Mainz, Johannes Gutenberg-Universit?t Mainz, Mainz, 55131, Germany|Padova University Hospital, Padova, 35128, Italy|University of Parma, Parma, 43126, Italy Less <<
NCT00862693 Glomerulonephritis|Autoimmune ... More >>Diseases Less << PHASE4 UNKNOWN 2025-03-11 Renal Division, Peking Univers... More >>ity First Hospital, Beijing, Beijing, 100034, China Less <<
NCT03216564 Diabetic Nephropathies PHASE3 UNKNOWN 2019-05-10 Hamad Medical Corporation, Doh... More >>a, Qatar Less <<
NCT03820518 X-linked Hypophosphatemia PHASE4 UNKNOWN 2022-12-31 Department of Endocrinology, P... More >>eking Union Medical College Hospital, Beijing, Beijing, 100730, China Less <<
NCT01293682 Breast Cancer PHASE2 COMPLETED 2025-12-21 University of Rochester, Roche... More >>ster, New York, 14642, United States Less <<
NCT05415254 COVID-19|Vitamin D Deficiency UNKNOWN 2022-09-19 Renji Hospital, Shanghai, Shan... More >>ghai, 200127, China Less <<
NCT00601328 Secondary Hyperparathyroidism|... More >>Hypocalcemia Less << COMPLETED 2025-08-03 Bio-Kinetic Clinical Applicati... More >>ons, Inc., Springfield, Missouri, 65801, United States Less <<
NCT01039181 Advanced Intrahepatic Cholangi... More >>ocarcinoma Less << PHASE2 UNKNOWN 2025-10-12 Srinagarind Hospital, Faculty ... More >>of Medicine, Khon Kaen University, Khon Kaen, 40002, Thailand Less <<
NCT01820832 Chronic Kidney Disease|Protein... More >>uria Less << PHASE4 UNKNOWN 2025-06-15 Huashan Hospital, Fudan Univer... More >>sity, Shanghai, Shanghai, 200040, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.00mL

2.40mL

1.20mL

24.00mL

4.80mL

2.40mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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