CHOLECALCIFEROL

CAS NUMBER: 67-97-0

EC NUMBER : 200-673-2

MOLECULAR FORMULA: C27H44O

MOLECULAR WEIGHT: 384.64

Cholecalciferol acts as a hormone precursor since it requires two stages of metabolism: first to 25-hydroxycholecalciferol; then to 1?, 25-dihydroxycholecalciferol.
One unit (U.S.P. or international) is defined as the activity of 0.025 µg of vitamin D3 contained in the USP vitamin D reference standard.

Cholecalciferol is sourced either through the diet or exposing skin to ultraviolet rays. 
Oral administration of vitamin D3 is readily absorbed and is stored in adipose tissue.

Cholecalciferol is made in the skin following UVB light exposure. 
Cholecalciferol is converted in the liver to calcifediol (25-hydroxyvitamin D) which is then converted in the kidney to calcitriol (1,25-dihydroxyvitamin D).
One of Cholecalciferol  actions is to increase the uptake of calcium by the intestines.

Cholecalciferol is found in food such as some fish, beef liver, eggs, and cheese. Certain foods such as milk, fruit juice, yogurt, and margarine also may have cholecalciferol added to them in some countries including the United States.
Cholecalciferol can be taken as an oral dietary supplement to prevent vitamin D deficiency or as a medication to treat associated diseases, including rickets. 

Cholecalciferol is also used for familial hypophosphatemia, hypoparathyroidism that is causing low blood calcium, and Fanconi syndrome.

Cholecalciferol supplements may not be effective in people with severe kidney disease. Excessive doses in humans can result in vomiting, constipation, weakness, and confusion. Other risks include kidney stones. Doses greater than 40,000 IU (1,000 µg) per day are generally required before high blood calcium occurs. Normal doses, 800–2000 IU per day, are safe in pregnancy.
Cholecalciferol was first described in 1936. 

Cholecalciferol is on the World Health Organization's List of Essential Medicines. In 2019, it was the 84th most commonly prescribed medication in the United States, with more than 9 million prescriptions.
Cholecalciferol is available as a generic medication and over the counter.

Cholecalciferol is also used at much higher doses to kill rodents
Cholecalciferol is a form of vitamin D which is naturally synthesized in skin and functions as a pro-hormone, being converted to calcitriol.
This is important for maintaining calcium levels and promoting bone health and development.

Cholecalciferol may be taken as a dietary supplement to prevent or to treat vitamin D deficiency. One gram is 40,000,000 (40x106) IU, equivalently 1 IU is 0.025 µg.
Cholecalciferol can be produced in skin from the light emitted by the UV lamps in tanning beds, which produce ultraviolet primarily in the UVA spectrum, but typically produce 4% to 10% of the total UV emissions as UVB. Levels in blood are higher in frequent uses of tanning salons.

Cholecalciferol and all forms of vitamin D are by definition "vitamins" can be disputed, since the definition of vitamins includes that the substance cannot be synthesized by the body and must be ingested. Cholecalciferol is synthesized by the body during UVB radiation exposure.
Cholecalciferol is one of the two major forms of vitamin D. It’s what your body naturally synthesizes in your skin during exposure to sunlight and it’s also a commercially prepared supplement made from the lanolin retrieved from washing lambs’ wool. 

Cholecalciferol - Which, as mentioned above, is formed naturally in the skin when exposed to sunlight, is present in significant levels in certain fish and eggs, and is also commercially made from lanolin washed from lambs’ wool. (New, vegan alternatives manufactured from lichen have also recently become available and Honest is exploring this as an option for our formulas.)

Cholecalciferol is approximately three times more potent than vitamin D2
Cholecalciferol  also binds to the protein receptors in your body much more effectively. This helps maintain levels in your circulatory system and more effectively increase blood level concentrations for optimal health.
Cholecalciferol is more bioavailable, meaning it’s more quickly and effectively converted and absorbed by your body. Some sources say it’s up to 500% faster than vitamin D2.

Cholecalciferol is an important chemical for both researchers and consumers.
Cholecalciferol  has a number of uses as Vitamin D3 in the production and creation of health supplements, as well as bone regrowth research and rodent pesticides. But before deciding to take a daily Vitamin D3 supplement or doing research on cholecalciferol, familiarize yourself with the specifics of this compound.

Cholecalciferol is naturally created in animal tissue. Ultraviolet-B radiation from sunlight begins the production of cholecalciferol by stimulating epidermal 7-dehydrocholesterol.
Cholecalciferol  is more similar to a hormone than a vitamin, which is usually required in a diet because it cannot be synthesized elsewhere in the body. It is structurally similar to steroids like testosterone, cortisol and cholesterol, despite being a secosteroid.

Cholecalciferol was registered for use as a rodenticide.
Cholecalciferol was a major ingredient in these pesticides made by the Dutch manufacturer Phillips-Dunphar and Wisconsin-based Bell Laboratories, the Environmental Protection Agency explained in a report. 

Cholecalciferol has been used primarily against Norway rats, roof rats, and house mice. When approved for this use, its toxicology on humans or the environment had not been heavily researched.
Cholecalciferol is most commonly used by consumers and medical researchers for bone and overall health.

Colecalciferol is a vitamin D supplement. It is prescribed if you have low vitamin D levels. 
Cholecalciferol is important for the absorption of calcium from your stomach and for the functioning of calcium in your body.
Colecalciferol is also available as a smaller dose in combination with alendronate, and is called Alendronic Acid/Colecalciferol tablets. These tablets are taken once weekly for osteoporosis.

Colecalciferol soft gelatin capsules contain soybean oil. Some medicines containing soybean oil might cause an allergic reaction in patients with a peanut or soy allergy. If you have a peanut or soy allergy, ensure that your doctor or pharmacist is aware of this and ask them to check your medicines

Cholecalciferol binds to vitamin D receptors and modulates gene expression. This leads to an increase in serum calcium concentrations by increasing intestinal absorption of phosphorus and calcium, promoting distal renal tubular reabsorption of calcium and increasing osteoclastic resorption.
Cholecalciferol (vitamin D3) is a fat-soluble steroid that is synthesized in the skin in the presence of ultraviolet light or obtained from the diet.

Cholecalciferol is known as vitamin D3 for historical reasons. The chemical structure of vitamin D2 was worked out earlier than that of D3 because of the availability of ergosterol, a sterol derived from fungus. UV light converts ergosterol to ergocalciferol, an analogue of cholecalciferol.
Cholecalciferol is known as vitamin D2 and equals vitamin D3 in preventing rickets. One international unit of vitamin D=0.025 µg; 400 IU or 10 µg of irradiated ergosterol are typically added per quart of milk. The US RDA (recommended dietary allowance) for vitamin D is 400 IU day-1. 

Cholecalciferol (vitamin D3) toxicosis in dogs and cats has occurred through ingestion of rodenticides containing cholecalciferol as the active ingredient. The effect of ingestion of large amounts of cholecalciferol is to increase the concentrations of calcium in the blood through increased bone resorption and intestinal transport (Dorman 1990).

Hypercalcemia due to cholecalciferol ingestion results in metastatic calcification of tissues throughout the body, particularly in the stomach, renal tubules, and blood vessels.
Cholecalciferol after absorption from the intestine is transported to the liver, where it is metabolized to 25-hydroxycholecalciferol by an NADPH-dependent reaction.
Cholecalciferol is physiologically produced in humans and other animals. The active form of vitamin D3 is 1,25-dihydroxycholecalciferol

Cholecalciferol  is chemically closely allied to the classical steroid hormones.
Cholecalciferol  can be produced photochemically by sunlight from a precursor, 7-dehydrocholesterol, present in the skin or alternatiavely obtained dietarily. Vitamin D3 is known to be metabolized into a family of over 30 daughter metabolites.

Cholecalciferol is known as vitamin D3 for historical reasons. The chemical structure of vitamin D2 was worked out earlier than that of D3 because of the availability of ergosterol, a sterol derived from fungus. UV light converts ergosterol to ergocalciferol, an analogue of cholecalciferol.

Cholecalciferol  is an important component of calcium and phosphate metabolism, ensuring, with PTH and FGF23, adequate serum concentrations of these two analytes for optimal cell function and bone mineralisation.
Cholecalciferol (vitamin D3) is the mammalian form of vitamin D. It is normally produced in the skin by the action of UV light on its precursor, 7- dehydrocholesterol. Essential amounts of the vitamin are obtained thus or from dietary sources such as fish oils.

USES OF CHOLECALCIFEROL:

Cholecalciferol (vitamin D3) is used as a dietary supplement when the amount of vitamin D in the diet is not enough. People most at risk for vitamin D deficiency are older adults, breastfed infants, people with dark skin, obese people, and those with limited sun exposure, or gastrointestinal disease (GI; affecting the stomach or intestines) such as Crohn's disease or celiac disease. 
Cholecalciferol is also used along with calcium to prevent and treat bone diseases such as rickets (softening and weakening of bones in children caused by lack of vitamin D), osteomalacia (softening and weakening of bones in adults caused by lack of vitamin D), and osteoporosis (a condition in which the bones become thin and weak and break easily).

Cholecalciferol (vitamin D3) is in a class of medications called vitamin D analogs. 
Cholecalciferol is needed by the body for healthy bones, muscles, nerves, and to support the immune system. 

Cholecalciferol is also used by helping the body to use more of the calcium found in foods or supplements.
Cholecalciferol is used as a dietary supplement in people who do not get enough vitamin D in their diets to maintain adequate health. 

Cholecalciferol may also be used for purposes not listed in this medication guide.
Cholecalciferol are more commonly found in individuals living in northern latitudes, or with other reasons for a lack of regular sun exposure, including being housebound, frail, elderly, obese, having darker skin, or wearing clothes that cover most of the skin. 

Cholecalciferol (vitamin D3) comes as a capsule, gel capsule, chewable gel (gummy), tablet, and liquid drops to take by mouth. 
Cholecalciferol is usually taken once or twice daily depending on the preparation, your age, and your medical condition(s).

Cholecalciferol is available without a prescription, but your doctor may prescribe cholecalciferol to treat certain conditions. Check with your doctor or pharmacist before taking a cholecalciferol (vitamin D) supplement. 

Use cholecalciferol at around the same time every day. Follow the directions on your product label or doctor's instructions carefully, and ask your doctor or pharmacist to explain any part you do not understand. 
Use cholecalciferol exactly as directed. Do not take more or less of it or take it more often than recommended by your doctor.

Cholecalciferol supplements are available alone and in combination with vitamins, and in combination with medications.There are conflicting reports concerning the relative effectiveness of cholecalciferol (D3) versus ergocalciferol (D2), with some studies suggesting less efficacy of D2, and others showing no difference. 
Cholecalciferol liquid drops may be added to your child's food or drink. 

There are differences in absorption, binding and inactivation of the two forms, with evidence usually favoring cholecalciferol in raising levels in blood, although more research is needed. 

A much less common use of cholecalciferol therapy in rickets utilizes a single large dose and has been called stoss therapy. Treatment is given either orally or by intramuscular injection of 300,000 IU (7,500 µg) to 500,000 IU (12,500 µg = 12.5 mg), in a single dose, or sometimes in two to four divided doses. There are concerns about the safety of such large doses.

Cholecalciferol is used as a dietary supplement in people who do not get enough vitamin D in their diets to maintain adequate health.
Cholecalciferol may also be used for purposes not listed in this medication guide

While using cholecalciferol, you will need frequent blood tests. You may also need x-rays.
Cholecalciferol is also used at much higher doses to kill rodents
Cholecalciferol is a form of vitamin D which is naturally synthesized in skin and functions as a pro-hormone, being converted to calcitriol.

This is important for maintaining calcium levels and promoting bone health and development.
Cholecalciferol is also used for familial hypophosphatemia, hypoparathyroidism that is causing low blood calcium, and Fanconi syndrome.

APPLICATION OF CHOLECALCIFEROL:

-Cholecalciferol helps your body absorb calcium. 

-Cholecalciferol is used as a dietary supplement in people who do not get enough vitamin D in their diets to maintain adequate health.

-Cholecalciferol is for purposes not listed in this medication guide.

-Low levels of Cholecalciferol  are more commonly found in individuals living in northern latitudes, or with other reasons for a lack of regular sun exposure, including being housebound, frail, elderly, obese, having darker skin, or wearing clothes that cover most of the skin.

PROPERTIES OF CHOLECALCIFEROL:

-Quality Level: 200

-Biological source: synthetic (organic)

-Assay: ?98% (HPLC)

-Form: powder

-Application(s): HPLC; suitable

-Color: white to off-white

-Melting Point: 83-86 °C (lit.)

-Storage temp.: 2-8°C

-Boiling Point:    496.4°C

-Solubility: Insoluble

STORAGE AND STABILITY OF CHOLECALCIFEROL:

Cholecalciferol C9756 is packaged under argon gas. If it is stored unopened at 2-8°C and protected from light
CHOLECALCIFEROL should be stable for a minimum of three years. Unused portions should be stored under nitrogen or argon gas. 
Deterioration is negligible after storage of one year in amber-evaculated ampules at refrigerator temperatures. It is oxidized and inactivated by moist air within a few days.

THE SYNTHESİS AND ACTİVATİON OF CHOLECALCIFEROL:

 -Cholecalciferol is synthesized in the skin from 7-dehydrocholesterol under the action of ultraviolet B (UVB) light. It reaches an equilibrium after several minutes depending on the intensity of the UVB in the sunlight - determined by latitude, season, cloud cover, and altitude - and the age and degree of pigmentation of the skin.

-Hydroxylation in the endoplasmic reticulum of liver hepatocytes of cholecalciferol to calcifediol (25-hydroxycholecalciferol) by 25-hydroxylase is loosely regulated, if at all, and blood levels of this molecule largely reflect the amount of cholecalciferol produced in the skin combined with any vitamin D2 or D3 ingested.

-Hydroxylation in the kidneys of calcifediol to calcitriol by 1-alpha-hydroxylase is tightly regulated: it is stimulated by parathyroid hormone and serves as the major control point in the production of the active circulating hormone calcitriol (1,25-dihydroxyvitamin D3).

BENEFITS:

-Cholecalciferol helps regulate and enable the absorption of mineral nutrients like calcium and phosphorus. It also helps regulate blood pressure and blood sugar levels.
Cholecalciferol is involved in the regulation of hormones related to stress, and optimal levels have been shown to help reduce conditions like seasonal affective disorder (SAD), depression, and anxiety.
Cholecalciferol acts as a macrophage in your bloodstream  large, specialized cells that are part of your immune system and attack foreign pathogens. Not only does it help defend against things like the cold and flu, but it’s also been shown to help prevent cancer.

MECHANİSM OF ACTİON:

By itself cholecalciferol is inactive.
Cholecalciferol is converted to its active form by two hydroxylations: the first in the liver, by CYP2R1 or CYP27A1, to form 25-hydroxycholecalciferol (calcifediol, 25-OH vitamin D3). The second hydroxylation occurs mainly in the kidney through the action of CYP27B1 to convert 25-OH vitamin D3 into 1,25-dihydroxycholecalciferol (calcitriol, 1,25-(OH)2vitamin D3).
All these metabolites are bound in blood to the vitamin D-binding protein. The action of calcitriol is mediated by the vitamin D receptor, a nuclear receptor which regulates the synthesis of hundreds of proteins and is present in virtually every cell in the body.

SYNONYMS:

-Calciol
-(+)-Vitamin D3
-7-Dehydrocholesterol activated
-Activated 7-dehydrocholesterol
-(1S,Z)-3-((E)-2-((1R,7AR)-7a-methyl-1-((R)-6-methylheptan-2-yl)hexahydro-1H-inden-4(2H)-ylidene)ethylidene)-4-methylenecyclohexanol
-(S)-4-Methylene-3-{2-[(R)-7a-(R)-methyl-1-((R)-5-methyl-1-methyl-hexyl)-octahydro-inden-(4E)-ylidene]-ethylidene}-cyclohexanol
-(1S,3Z)-3-{2-[(1R,4E,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexan-1-ol
-(1S,3Z)-3-[(2E)-2-[(1R,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexan-1-ol