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Doxercalciferol Vitamin chemical

Cat.No.S1467

Doxercalciferol (1α-hydroxyvitamin D2) is a synthetic vitamin D2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.
Doxercalciferol Vitamin chemical Chemical Structure

Chemical Structure

Molecular Weight: 412.65

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 412.65 Formula

C28H44O2

Storage (From the date of receipt)
CAS No. 54573-75-0 Download SDF Storage of Stock Solutions

Synonyms 1α-hydroxyvitamin D2 Smiles CC(C)C(C)C=CC(C)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (201.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 70 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

In vivo
Doxercalciferol (100 or 300 pg/g b.w.) normalizes serum calcium and parathyroid hormone (PTH) levels in nephrectomy treated mice. This compound (300 pg/g b.w.) significantly reduces osteitis fibrosa in nephrectomy treated mice. [1] It results in significant decrease in cardiac hypertrophy and improves cardiac function in rats fed a high salt (HS) diet. This treatment leads to a significant decrease in plasma brain natriuretic peptide (BNP) level and tissue atrial natriuretic factor (ANF) mRNA level in rats fed a high salt (HS) diet. It also significantly reduces the level of protein kinase C-α (PKCα) suggesting that PKC-mediated cardiac hypertrophy may be associated with vitamin D deficiency. [2] This chemical decreases proteinuria, podocyte injury, mesangial expansion, and extracellular matrix protein accumulation in Diet-induced obesity (DIO) mice. It also decreases macrophage infiltration, oxidative stress, proinflammatory cytokines, and profibrotic growth factors in DIO mice. It also prevents the activation of the renin-angiotensin-aldosterone system including the angiotensin II type 1 receptor and the mineralocorticoid receptor in DIO mice. [3] This compound combined with Losartan most effectively prevents albuminuria, restored glomerular filtration barrier structure, and dramatically reduces glomerulosclerosis in a dose-dependent manner in mice. This combination virtually prevents morphological and molecular changes in diabetic kidneys of mice. [4]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00792857 Completed
Chronic Kidney Disease|Secondary Hyperparathyroidism|Chronic Renal Insufficiency|Chronic Renal Failure
OPKO IP Holdings II Inc.|OPKO Health Inc.
November 2008 Phase 1

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