中文名 | Lexacalcitol |
英文名 | Lexacalcitol |
别名 | 来沙骨化醇 化合物 T15745 |
英文别名 | KH 106 KH 1060 Lexacalcitol Lenosacalcitol Lexacalcideferol (1S*,3R*,5Z),7aalpha))-(5Z,7E,20R)-20-((4-Ethyl-4-hydroxyhexyl)oxy)-9,10-secopregna-5,7,10(19)-triene-1alpha,3beta-diol 1,3-Cyclohexanediol, 5-[(2E)-2-[(1S,3aS,7aS)-1-[(1R)-1-[(4-ethyl-4-hydroxyhexyl)oxy]ethyl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-, (1R,3S,5Z)- (1R,3S,5Z)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(1R)-1-(4-ethyl-4-hydroxyhexoxy)ethyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol |
CAS | |
化学式 | C29 H48 O4 |
分子量 | 460.69 |
密度 | 1.07±0.1 g/cm3(Predicted) |
沸点 | 600.3±55.0 °C(Predicted) |
酸度系数 | 14.43±0.40(Predicted) |
存储条件 | -20℃ |
体外研究 | Lexacalcitol inhibits cell proliferation by 50% at 10 -12 M (14,000 times more active than la,25(OH) 2 D 3 ) in human histiocytic lymphoma cell line U 937. Lexacalcitol inhibits interleukin-1-induced mouse thymocyte proliferation by 50% at 3×10 -16 M , allogeneic stimulation of mouse spleen lymphocytes at 5×10 -15 M. |
体内研究 | Lexacalcitol (0.5 mg/kg/2 days; i.p.) in combination with cyclosporin A (CyA) can prevent autoimmune destruction of syngeneic islet grafts in spontaneously diabetic NOD recipients. Animal Model: Male and female spontaneously diabetic NOD mice Dosage: 0.5 mg/kg/2 days Administration: Intraperitoneal injection Result: Single treatment with KH1060 or CyA did not result in statistically significant suppression of early graft failure, while the combination of KH1060 and CyA can prevent early graft failure and delay graft rejection of xenogeneic islets in spontaneously diabetic NOD mice. |
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