Cholecalciferol

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Cat Number

API0231520

CAS Number

67-97-0

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Product Detail Description Scientific Support Customer Q&A

CAS Number

67-97-0

EINECS

200-673-2

Storage

Store at 2-8℃

Synonyms

Vitamin D3; Colecalciferol; Calciol; Oleovitamin D3; Ricketon; Deparal; Arachitol; Delsterol

Molecular Formula

C27H44O

Molecular Weight

384.6

Smiles

C[C@H](CCCC(C)C)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](CCC3=C)O)C

Appearance

White to off-white powder

Melting Point

83-86℃

Boiling Point

451℃

General Description

Cholecalciferol, or vitamin D3, is a fat-soluble secosteroid synthesized in the skin upon exposure to ultraviolet B radiation and obtained from dietary sources. It is the preferred form of vitamin D for supplementation due to its superior bioavailability compared to ergocalciferol. This agent is available in a wide range of over-the-counter and prescription strengths for the management of vitamin D insufficiency.

Mechanism of Action

Cholecalciferol undergoes sequential hydroxylation in the liver to calcifediol and subsequently in the kidney to calcitriol, the biologically active hormone. Calcitriol binds to intracellular vitamin D receptors, facilitating the transcription of genes that regulate calcium absorption in the gut, bone mineralization, and parathyroid hormone suppression. This endocrine pathway maintains serum calcium levels within a narrow physiological range.

Application

It is indicated for the treatment and prevention of vitamin D deficiency, nutritional rickets, and osteomalacia, as well as an adjunct in the management of osteoporosis. Supplementation is routinely recommended for elderly individuals, breastfed infants, and patients with limited sun exposure or conditions impairing fat absorption. Dosing regimens range from daily low-dose maintenance to high-dose intermittent therapy for severe deficiency states.

A 2‑year double‑blind trial randomized 181 patients with relapsing‑remitting MS and low serum 25(OH)D (<75 nmol/L) to high‑dose oral cholecalciferol 100,000 IU or placebo every other week, added to interferon beta‑1a. The primary endpoint—annualized relapse rate at 96 weeks—was not met. However, among completers (45 per group), all efficacy parameters favored cholecalciferol: reduced ARR (p=0.012), fewer new T1 hypointense lesions (p=0.025), lower T1 lesion volume (p=0.031), and less EDSS progression (p=0.026). Adverse events were balanced. Although the primary endpoint was negative, secondary outcomes suggest potential benefit warranting further exploration.

Fig. 1 Trial flowchart. (Camu W, et al., 2019)

References

Camu W, et al. Cholecalciferol in relapsing-remitting MS: A randomized clinical trial (CHOLINE). Neurol Neuroimmunol Neuroinflamm. 2019; 6(5):e597.

Does Cholecalciferol require strict protection from light and air?

Yes, it is extremely sensitive to light, oxygen, and heat. Storage in light-resistant, airtight containers, preferably under nitrogen, at 2-8°C is required.

What is the recommended storage temperature for Cholecalciferol?

Store at 2-8°C. At room temperature, it rapidly degrades, forming pre-vitamin D and other photoisomers, leading to significant potency loss.

Is Cholecalciferol stable in powder blends for multivitamin formulations?

It can be stabilized by using antioxidants and by protecting the blend from light and moisture. We provide formulation guidance for maintaining stability in solid dosage forms.

How is the purity of Cholecalciferol monitored during stability studies?

We use a stability-indicating HPLC method to monitor for degradation products, including trans-cholecalciferol and isotachysterol, ensuring they remain within acceptable limits.