1α,25-dihydroxycholecalciferol
1A,25-dihydroxycholecalciferol
CAS: 32222-06-3
Molecular Formula: C27H44O3
1α,25-dihydroxycholecalciferol - Names and Identifiers
1α,25-dihydroxycholecalciferol - Physico-chemical Properties
| Molecular Formula | C27H44O3 |
| Molar Mass | 416.64 |
| Density | 1.0362 (rough estimate) |
| Melting Point | 119-1210C |
| Boling Point | 474.91°C (rough estimate) |
| Specific Rotation(α) | D25 +48° (methanol) |
| Flash Point | 14 °C |
| Solubility | Insoluble in water |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White crystalline powder |
| Color | White to Almost white |
| Maximum wavelength(λmax) | ['265nm(lit.)'] |
| Merck | 14,1644 |
| BRN | 7559394 |
| pKa | 14.43±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Air and Light Sensitive |
| Sensitive | Air and light sensitivity |
| Refractive Index | 1.4700 (estimate) |
| MDL | MFCD00867079 |
| Use | Renal osteodystrophy in patients with chronic renal failure |
| In vitro study | Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, inhibiting 70% of tritiated thymidine incorporation after 72 h of culture. Calcitriol inhibits interleukin-2 (IL-2) production in PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent manner. Calcitriol increases intracellular calcium ion concentration within 5 seconds by mobilizing calcium from the endoplasmic reticulum and inositol 1,4, 5-trisphosphate and Diglyceride formation. Calcitriol can inhibit the proliferation of human prostate adenocarcinoma cells and promote the differentiation of human prostate adenocarcinoma cells. Calcitriol selectively reduces the secretion level of type IV collagenase (MMP-2 and MMP-9). In squamous cell carcinoma and prostate cancer, Calcitriol has antiproliferative activity and enhances the antitumor activity of platinum-based drugs. In mouse squamous cell carcinoma and PC-3 cells, Calcitriol has a stronger effect than paclitaxel, reducing clonal survival. Calcitriol is a potent antiproliferative agent in a variety of malignant cell types. Calcitriol acts by increasing G0/G1 phase arrest, inducing apoptosis and differentiation, and regulating the expression of growth factor receptors. Calcitriol promotes the antitumor effects of many cytotoxic agents and inhibits the invasiveness of tumor cells and the formation of new blood vessels. |
1α,25-dihydroxycholecalciferol - Risk and Safety
| Risk Codes | R26/27/28 - Very toxic by inhalation, in contact with skin and if swallowed. R63 - Possible risk of harm to the unborn child R36/37/38 - Irritating to eyes, respiratory system and skin. R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S16 - Keep away from sources of ignition. S7 - Keep container tightly closed. |
| UN IDs | UN 2811 6.1/PG 1 |
| WGK Germany | 3 |
| RTECS | FZ4645000 |
| FLUKA BRAND F CODES | 8-10-19 |
| HS Code | 29061900 |
| Hazard Class | 6.1(a) |
| Packing Group | I |
1α,25-dihydroxycholecalciferol - Reference Information
| introduction | dihydroxycholecalciferol is one of the most important active metabolites of vitamin 1 α,25-D3. This metabolite is usually formed in the kidney. In recent years, it has been found that calcitriol can also be produced outside the kidney. It has been confirmed that the placenta, monocytes, macrophages, tumor cell supernatants, lymph nodes and keratinocytes of patients with sarcoidosis all have 1α hydroxylase and can produce calcitriol. The precursor of calcitriol is 25-hydroxy cholecalciferol (alfaecalcidol). Dihydroxycholecalciferol can promote the absorption of calcium in the small intestine and regulate the transport of inorganic salts in bone. |
| indications | suitable for renal malnutrition, hypoparathyroidism, vitamin d-dependent rickets and vitamin d-resistant rickets in patients with chronic renal failure. |
| Physiological effects | Calcitriol, also known as calcitriol, is the active form of vitamin D and a hormone in the body. It plays an important role in regulating blood calcium and blood phosphorus concentration. It can increase the calcium level in the blood by increasing the absorption of calcium ions in the intestine, and can increase the release of calcium in the bone to increase the blood calcium level, this study was first reported by Michael F. Holick in 1971. The principle of action of calcitriol is in many cases through binding to the vitamin D receptor (VDR). For example, the ligand-receptor complex formed by the receptor in the cytoplasm of small intestinal epithelial cells and calcitriol is transferred to the nucleus. As a transcription factor that promotes the expression of calcium-binding protein coding genes, the increase of calcium-binding protein enables cells to actively transport more calcium ions, thereby increasing the level of calcium ion absorption. Absorbing calcium ions also needs to transport anions to maintain electrical neutrality, mainly by absorbing inorganic phosphate ions, so calcium triol also promotes the absorption of phosphorus. clinically, this medicine can be used to treat hypocalcemia, hypoparathyroidism (adults), osteomalacia, rickets (infants), chronic kidney disease, renal bone disease, osteoporosis, and prevent osteoporosis caused by glucocorticoids. Calcitriol stereolecular formula |
| biological activity | Calcitriol (RO215535, Topitriol, 1,25-Dihydroxyvitamin D3), as a hormone active form of vitamin d, is an activator of non-selective vitamin d receptor, and its binding affinity to vitamin d receptor (IC50=0.4 nM) is more than 10 times that of selective VDRA paricalcitol. It is recommended to use it now. |
| Target | Value |
| use | vitamin drugs. For renal osteodystrophy in patients with chronic renal failure. |
| category | toxic substances |
| toxicity classification | highly toxic |
| acute toxicity | oral administration-rat LD50 0.62 mg/kg; Oral administration-mouse LD50: 1.35 mg/kg |
| flammability hazard characteristics | combustible, spicy and irritating smoke from the fire site |
| storage and transportation characteristics | warehouse ventilation and low temperature drying; separate from food storage and transportation |
| fire extinguishing agent | water, sand |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-10 22:30:50
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