156965-15-0
156965-15-0 结构式
基本信息
中文别名
胆钙化醇杂质21(维生素D3杂质21) 英文别名
ZK-15922ZK 159222
SPARTCPUGRJFRS-PBDCIXLPSA-N
Cholecalciferol Impurity 21
Cyclopropanecarboxylic acid, 1-[(1R,2E,4R)-4-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylenecyclohexylidene]ethylidene]octahydro-7a-methyl-1H-inden-1-yl]-1-hydroxy-2-penten-1-yl]-, butyl ester
物理化学性质
熔点>62°C (dec.)
沸点646.3±55.0 °C(Predicted)
密度1.13±0.1 g/cm3(Predicted)
储存条件Amber Vial, -86°C Freezer, Under inert atmosphere
溶解度可溶于氯仿(少许)、乙酸乙酯(少许)、甲醇(少许)
酸度系数(pKa)14.29±0.20(Predicted)
形态固体
颜色灰白色至浅灰色
稳定性对光敏感、对温度敏感
常见问题列表
生物活性
ZK159222 是 1α,25-(OH)2D3 的类似物,是有效的 1α,25-(OH)2D3 受体 (VDR) 拮抗剂。ZK159222 拮抗作用的机制是由配体诱导的维生素 D 受体与辅助激活剂的相互作用缺乏所介导的。ZK159222 具有部分激动性。体外研究
ZK159222, displayed the profile of a weak VDR agonists that requires an approximate 7-fold higher concentration than of the natural hormone 1α,25-(OH)2D3 to stabilize VDR-RXR heterodimer complex formation on a DR3-type VDRE. ZK159222 was found to belong to the category of 1α,25-(OH)2D3 analogues that stabilize an additional third functional VDR conformation, which has also been described for some agonistic 20-epi analogues. The remaining reporter gene activity that was obtained by a combined treatment of 10 nM 1α,25-(OH)2D3 with 1 μM ZK159222 is close to the partial agonistic activity of 1 μM ZK159222.