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Doxercalciferol

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Chemical Structure| 54573-75-0 同义名 : 1.alpha.-Hydroxyvitamin D2;1-hydroxy Vitamin D2;Doxercalciferol. 1-hydroxy Vitamin D2;TSA 840;1-Hydroxyergocalciferol;Hectorol;1α-hydroxyvitamin D2
CAS号 : 54573-75-0
货号 : A580119
分子式 : C28H44O2
纯度 : 99%+
分子量 : 412.648
MDL号 : MFCD00871065
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(254.45 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Doxercalciferol (DOX) is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease. DOX had a beneficial effect on age-related bone deteriorations in aging mice by promoting osteoblast activity and cartilage regeneration and inhibiting osteoclast-specific genes expression[3]. Doxercalciferol (0.083, 0.167 or 0.333 μg/kg, i.p.) elevates serum phosphorus at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol (0.167 and 0.333 μg/kg) also increases serum calcium and Ca × P at Weeks 2 and 6, and enhances increased pulse wave velocity (PWV) at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol blocks PTH from rising at 0.083 μg/kg, and lowers serum PTH to the SHAM level[4]. Doxercalciferol was administered intraperitoneally at 150 ng, 3 times per week (Monday, Wednesday, Friday) for 6 weeks. Rats on HS diet with doxercalciferol administration had significant decrease in cardiac hypertrophy and improved cardiac function compared to the HS + vehicle. In addition, there was a significant decrease in plasma brain natriuretic peptide (BNP) level and tissue atrial natriuretic factor (ANF) mRNA level with doxercalciferol treatment. Doxercalciferol also significantly reduced the level of protein kinase C-α (PKCα)[5]. Doxercalciferol (125 ng/kg, i.p. thrice per week) increases expression of VDR mRNA level and renal expression of TRPV5 in NON mice fed a HF diet. Doxercalciferol also improves proteinuria, prevents loss of podocytes, and accumulation of extracellular matrix proteins in HF diet-induced mice[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01717989 - Completed - -
NCT01717989 - Completed - -
NCT01181531 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.23mL

4.85mL

2.42mL
参考文献

[1]St-Arnaud R, Arabian A, et al. Differential effects of oral doxercalciferol (Hectorol) or paricalcitol (Zemplar) in the Cyp27b1-null mouse model of uremia. Nephron Exp Nephrol. 2011;119(3):e67-74.

[2]Choi JH, Ke Q, et al. Doxercalciferol, a pro-hormone of vitamin D, prevents the development of cardiac hypertrophy in rats. J Card Fail. 2011 Dec;17(12):1051-8.

[3]Li J, Li N, Yan S, Liu M, Sun B, Lu Y, Shao Y. Doxercalciferol Alleviates Bone Deteriorations and Cartilage Degeneration in Aging Mice. Exp Clin Endocrinol Diabetes. 2020 Aug;128(8):540-547

[4]Noonan W, Koch K, Nakane M, Ma J, Dixon D, Bolin A, Reinhart G. Differential effects of vitamin D receptor activators on aortic calcification and pulse wave velocity in uraemic rats. Nephrol Dial Transplant. 2008 Dec;23(12):3824-30

[5]Choi JH, Ke Q, Bae S, Lee JY, Kim YJ, Kim UK, Arbeeny C, Thadhani R, Kang PM. Doxercalciferol, a pro-hormone of vitamin D, prevents the development of cardiac hypertrophy in rats. J Card Fail. 2011 Dec;17(12):1051-8

[6]Wang XX, Jiang T, Shen Y, Santamaria H, Solis N, Arbeeny C, Levi M. Vitamin D receptor agonist doxercalciferol modulates dietary fat-induced renal disease and renal lipid metabolism. Am J Physiol Renal Physiol. 2011 Mar;300(3):F801-10