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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Purity: ≥98%
Calcitriol (RO215535, Topitriol; 1,25(OH)2D3) is an agonist of the vitamin D receptor (VDR) and the form of vitamin D that is metabolically and hormonally active. When calcitriol is converted, it produces metabolites that are more powerful and act faster than other vitamin D forms. Calcitriol regulates the differentiation, growth, and function of the cell immune system, which plays a major role in maintaining mineral and skeletal homeostasis. Studies conducted in vitro have revealed that calcitriol can inhibit the production of interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) in human peripheral blood cells (PBMC) stimulated by lipopolysaccharide (LPS) in a dose-dependent manner.
Targets |
Human Endogenous Metabolite
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ln Vitro |
Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, achieving 70% suppression of tritiated thymidine incorporation after 72 hours in culture. In a concentration-dependent manner, calcitriol reduces the production of interleukin-2 (IL-2) by PHA-stimulated peripheral blood mononuclear cells.[1]
Calcitriol increases the intracellular calcium concentration ([Ca2+]i) in less than 5 seconds by causing the endoplasmic reticulum to release calcium and forming inositol 1,4, 5-trisphosphate and diacylglycerol.[2] Calcitriol can both stimulate and prevent the growth of human prostate adenocarcinoma cells. Type IV collagenases' (MMP-2 and MMP-9) secreted levels are selectively decreased by calcitriol.[3] Calcitriol increases the antitumor activity of platinum-based drugs and exhibits antiproliferative activity in prostatic adenocarcinoma and squamous cell carcinoma. In PC-3 and murine squamous cell carcinoma cells, calcitriol prior to paclitaxel significantly lowers clonogenic survival compared with either agent alone.[4] Calcitriol is a potent anti-proliferative agent that targets a broad range of cancerous cell types. Growth factor receptor expression is modulated, apoptosis and differentiation are induced, and G0/G1 arrest is increased in response to calcitriol. Calcitriol inhibits the motility and invasiveness of tumor cells as well as the development of new blood vessels, thereby amplifying the antitumor effects of numerous cytotoxic agents.[5] |
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ln Vivo |
Calcitriol treatment (150 ng/kg per day for 4.5 months) improves relaxations (pD2: 6.30±0.09, Emax: 68.6±3.9% in OVX treated with Calcitriol, n=8). Both kidneys of OVX rats have decreased renal blood flow, which is remedied by calcitriol treatment. Chronic calcitriol administration decreases the increased expression of Thromboxane-prostanoid (TP) receptor and COX-2 in the renal arteries of OVX rats[3]. Treatment with high- and low-dose calcitriol reduces the fructose-fed rats' systolic blood pressure (SBP) by 14±4 and 9±4 mmHg, respectively, on day 56. When compared to other groups, high-dose calcitriol treatment (20 ng/kg per day) significantly raises serum ionized calcium levels (1.44±0.05 mmol/L).
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Cell Assay |
Calcitriol (100 nM) or DMSO (vehicle control) were used to treat CLL cells. At the designated time intervals, cells were harvested with a light trypsinization.
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Animal Protocol |
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References |
Molecular Formula |
C27H44O3
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Molecular Weight |
416.64
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Exact Mass |
416.33
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Elemental Analysis |
C, 77.84; H, 10.65; O, 11.52
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CAS # |
32222-06-3
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Appearance |
Solid powder
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SMILES |
C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](C[C@@H](C3=C)O)O)C
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InChi Key |
GMRQFYUYWCNGIN-NKMMMXOESA-N
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InChi Code |
InChI=1S/C27H44O3/c1-18(8-6-14-26(3,4)30)23-12-13-24-20(9-7-15-27(23,24)5)10-11-21-16-22(28)17-25(29)19(21)2/h10-11,18,22-25,28-30H,2,6-9,12-17H2,1,3-5H3/b20-10+,21-11-/t18-,22-,23-,24+,25+,27-/m1/s1
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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
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4002 mL | 12.0008 mL | 24.0015 mL | |
5 mM | 0.4800 mL | 2.4002 mL | 4.8003 mL | |
10 mM | 0.2400 mL | 1.2001 mL | 2.4002 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05415254 | Recruiting | Drug: Calcitriol | COVID-19 Vitamin D Deficiency |
RenJi Hospital | June 12, 2022 | Not Applicable |
NCT03748966 | Recruiting | Drug: Calcitriol | X-linked Hypophosphatemia Hypophosphatemic Rickets |
Massachusetts General Hospital | March 28, 2019 | Early Phase 1 |
NCT05902078 | Not yet recruiting | Drug: Eldecalcitol capsules Drug: Calcitriol capsules |
Low Bone Mineral Density Postmenopausal Osteoporosis |
Shanghai Jiao Tong University Affiliated Sixth People's Hospital |
June 2023 | Phase 4 |
NCT05298163 | Not yet recruiting | Drug: Calcitriol capsules Drug: Placebo |
Diabetic Kidney Disease | Indonesia University | April 2022 | Not Applicable |
NCT02859896 | Active Recruiting |
Drug: Doxercalciferol (GZ427397) Drug: Calcitriol |
Secondary Hyperparathyroidism -Chronic Kidney Disease |
Sanofi | Phase 3 | Phase 3 |
Calcipotriol inducedERαexpression in ER-negative breast cancer cells. Calcitriol induced ERαprotein expression.BMC Cancer.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230. th> |
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Immunocytochemical analysis of ERαand VDR in primary and established breast cancer cells.BMC Cancer.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230. Calcitriol induced a fully active ERα.BMC Cancer.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230. td> |
Calcitriol inducedERαmRNA expression through the VDR in ERα-negative breast cancer cells.BMC Cancer.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230. td> |