Doxercalciferol 是一种维生素 D2 类似物,是一种维生素 D 受体激活剂,能够阻碍肾病的进程。
产品描述
Doxercalciferol is a synthetic vitamin D2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.
体内活性
Doxercalciferol (100 or 300 pg/g b.w.) normalizes serum calcium and parathyroid hormone (PTH) levels in nephrectomy treated mice. Doxercalciferol (300 pg/g b.w.) significantly reduces osteitis fibrosa in nephrectomy treated mice. [1] Doxercalciferol results in significant decrease in cardiac hypertrophy and improves cardiac function in rats fed a high salt (HS) diet. Doxercalciferol 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. Doxercalciferol 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] Doxercalciferol decreases proteinuria, podocyte injury, mesangial expansion, and extracellular matrix protein accumulation in Diet-induced obesity (DIO) mice. Doxercalciferol also decreases macrophage infiltration, oxidative stress, proinflammatory cytokines, and profibrotic growth factors in DIO mice. Doxercalciferol 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] Doxercalciferol combined with Losartan most effectively prevents albuminuria, restored glomerular filtration barrier structure, and dramatically reduces glomerulosclerosis in a dose-dependent manner in mice. Doxercalciferol combined with Losartan virtually prevents morphological and molecular changes in diabetic kidneys of mice. [4]
Cas No.
54573-75-0
分子式
C28H44O2
分子量
412.658
别名
1α-hydroxyvitamin D2;Hectorol;TSA 840;1.alpha.-Hydroxyvitamin D2;度骨化醇;Doxercalciferol
储存和溶解度
Ethanol:20.6 mg/mL (50 mM)
DMSO:4.1 mg/mL (10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years