度骨化醇 T6112

Product Introduction
Bioactivity


英文名: Doxercalciferol

描述: Doxercalciferol (TSA 840) 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。

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 20.6 mg/mL (50 mM)
DMSO : 4.1 mg/mL (10 mM)


关键字: TSA840 | Doxercalciferol | 1a-hydroxyvitamin D2 | Vitamin D receptor | 1alpha-hydroxyvitamin D2 | inhibit | Inhibitor | Vitamin D | TSA-840 | VD/VDR

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Nuclear Receptor Compound Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途