西奥骨化醇

中文名称:

西奥骨化醇

中文同义词:

西奥骨化醇

英文名称:

Seocalcitol

英文同义词:

(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4E)-6-Ethyl-6-hydroxy-1-methyl-2,4-octadien-1-yl]-octahydro-7α-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-1,3-cyclohexanediol;Seocalcitol;(1R,3S,5Z)-5-((2E)-((1R,3aS,7aR)-1-((1R,2E,4E)-6-Ethyl-6-hydroxy-1-methyl-2,4-octadienyl)octahydro-7a-methyl-4H-inden-4-ylidene)ethylidene)-4-methylene-1,3-cyclohexanediol;EB 1089,(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4E)-6-Ethyl-6-hydroxy-1-methyl-2,4-octadien-1-yl]-octahydro-7α-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-1,3-cyclohexanediol;1,3-Cyclohexanediol, 5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4E)-6-ethyl-6-hydroxy-1-methyl-2,4-octadien-1-yl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-, (1R,3S,5Z)-

CAS号:

134404-52-7

分子式:

C30H46O3

分子量:

454.68

EINECS号:

相关类别:

原料药

Mol文件:

134404-52-7.mol

熔点 

123-125°

沸点 

608.5±55.0 °C(Predicted)

密度 

1.06±0.1 g/cm3(Predicted)

储存条件 

Store at -20°C

酸度系数(pKa)

14.29±0.29(Predicted)

生物活性

Seocalcitol 是一种 vitamin D 类似物，作用于人骨肉瘤 MG-63 细胞，结合 vitamin D 受体蛋白，Kd 为 0.27 nM。

靶点

Kd: 0.27 nM (vitamin D receptor)

体外研究

Seocalcitol (EB 1089) is a stimulators of osteoclast recruitment in murine bone marrow cultures, with EC 50 at 0.1 nM. Seocalcitol stimulates bone resorption with an estimated EC 50 at 0.03 nM. Seocalcitol (EB 1089) elicites a dose-dependent induction of 24-hydroxylase mRNA in the kidney (EC 50 =0.4±0.13). In the kidney, K d values for Seocalcitol is 0.48±0.04 nM. However, in the intestine, the K d for Seocalcitol is 1.43±0.19 nM). Seocalcitol (0.1-10 nM) induces cell differentiation in a dosedependent manner. A higher differentiating activity is observed for 1 nM Seocalcitol (EB 1089) than for 1 nM VD 3 .

体内研究

Seocalcitol (EB1089), a synthetic vitamin D analog, exhibits reduced hypercalcemic activity relative to 1,25(OH) 2 VD 3 . In another study, long-term intraperitoneal (IP) administration of Seocalcitol at a dose of 0.5 μg/kg body weight every other day in C3H/Sy mice exertes a very strong inhibitory effect on hepatocellular carcinoma (HCC) development. Seocalcitol (EB 1089) is administered daily to postnatal rats from 4 to 12 days of age (P4 to P12) by intraperitoneal injection at either 0.38 or 1.25 μg/kg body weight (BW)/day. Only the highest dose of Seocalcitol (1.25 μg/kg BW) causes a significant reduction in weight gain when administered alone or in conjunction with Dexamethasone, all-trans retinoic acid (RA), or retinoic acid.