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What is Vitamin D Derivative Drugs?
Active vitamin D drugs are a general term for a series of vitamin D2/D3 derivatives, commonly referred to as "calciferol" drugs. These compounds are complex in structure and involve techniques such as photochemistry and microbial transformation. They are difficult to synthesize, sensitive to light and oxygen, and the API in the preparation is microgram-level, and the development threshold is high. Clinically used mainly for the treatment of osteoporosis, secondary hyperparathyroidism and psoriasis.
Calcitriol is the active form of vitamin D and is also a kind of hormones in the body. It plays an important role in the regulation of calcium and phosphorus concentration. It can increase the blood calcium level by increasing the intestinal absorption of calcium and can also increase the release of the bone calcium release for increasing the blood calcium levels. This study was first conducted and reported by Michael F. Holick in 1971. The basic principle of action model of calcitriol in many cases is through binding with the vitamin D receptor (the VDR), e.g., the ligand-receptor complex forming between calcitriol and its receptor in the intestinal epithelial cells cytoplasm can be transferred to the nucleus for being as the transcriptional factor in promoting the expression of calcium-binding protein. The increased level of calcium-binding proteins can help the cell to actively transport of more calcium ions, thereby increasing the calcium absorption level. Calcium absorption while maintaining electrical neutrality also requires transporting anions, mainly the absorption of inorganic phosphate ions, so calcitriol also promote the absorption of phosphorus.
Clinically, this drug can be used in the treatment of hypocalcemia, hypoparathyroidism (adult), osteomalacia, rickets (infants), chronic kidney disease, renal osteodystrophy, osteoporosis, as well as the prevention of glucocorticoid induced osteoporosis.
Basic Information
Product Name: | Calcitriol |
Synonyms: | Calcitriol Impurity; Vitamin D, 1α, 25-Dihydroxy- - CAS 32222-06-3 - Calbiochem; (5z,7e)-9,10-secocholesta-5,7,10(19)-triene-1-alpha,3-beta,25-triol; 1,25-dhcc; 1,25-dihydroxycholecalciferol; 1,25-dihydroxyvitamind; 1a,25-dihydroxy-cholecalcifero; 1-alpha,25-dihydroxy-cholecalcifero |
CAS: | 32222-06-3 |
MF: | C27H44O3 |
MW: | 416.64 |
EINECS: | 250-963-8 |
Product Categories: | Miscellaneous Biochemicals;Vitamin D3 analogs;API;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors;Isolabel;reagent;standard substance |
Quality Standard: | USP9.0 |
Molecular Structure: |
Melting point | 119-1210C |
Alpha | D25 +48° (m'ethanol) |
Boiling point | 474.91°C (rough estimate) |
Density | 1.0362 (rough estimate) |
Refractive index | 1.4700 (estimate) |
Fp | 14 °C |
Storage temp. | 2-8°C |
λmax | 265nm(lit.) |
Merck | 14,1644 |
BRN | 7559394 |
Stability: | Air and Light Sensitive |
Uses
1)Calcium regulator, anti-psoriatic;
2)Vitamin medicines; it can be used for treating the renal bone malnutrition of patients with chronic renal failure;
3)The biologically active form of vitamin D3. Calcium regulator; vitamin (antirachitic); antihyperparathyroid; antineoplastic; antipsoriatic
4)Calcitriol (1α,25-dihydroxy Vitamin D3) is synthesized from 7-dehydrocholesterol in humans via a non-enzymatic photochemical reaction with 290-310 nm UV light in the skin. Hydroxylation of the resulting cholecalciferol in the liver produces 25-hydroxy Vitamin D3, the principal circulating form of Vitamin D. A second, tightly regulated hydroxylation in the kidney produces calcitriol. Plasma calcitriol levels range from 10-70 pg/ml and are influenced by numerous dietary and hormonal factors. The main physiologic effects of calcitriol are to increase the absorption of calcium at the level of the intestinal epithelium, and to increase the mineralization of bone via the direct stimulation of osteoblasts.