(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one
- CAS号:173388-20-0
- 英文名:(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one
- 中文名:(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one
- CBNumber:CB73864466
- 分子式:C27H38O4
- 分子量:426.59
- MOL File:173388-20-0.mol
- 沸点 :618.5±55.0 °C(Predicted)
- 密度 :1.14±0.1 g/cm3(Predicted)
- 储存条件 :4°C, protect from light, stored under nitrogen
- 溶解度 :Soluble in ethanol
- 酸度系数(pKa) :14.43±0.40(Predicted)
- 形态 :Solid
- 颜色 :White to yellow
(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one性质、用途与生产工艺
- 生物活性 TEI-9647 是一种 Vitamin D3 Lactone 类似物,是一种有效的,特异性的维生素 D 受体 (VDR) 拮抗剂。 TEI-9647 抑制 VDR/VDRE 介导的 1α,25(OH)2D3 的基因组作用。TEI-9647 可以抑制 1α,25(OH)2D3 诱导的骨吸收和 HL-60 细胞分化。TEI-9647 有潜力用于抑制 Paget 病中过度的骨吸收和破骨细胞形成。
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体外研究
TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21 WAF1,CIP1 gene expression induced by 1α,25(OH) 2 D 3 .
TEI-9647 (10-1000 nM; 96 hours) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH) 2 D 3 . TEI-9647 completely blocks the increase in CD11b and the decrease in CD71 expression at 100 nM.
TEI-9647 blocks both 1α,25(OH) 2 D 3 -mediated HL-60 cell differentiation and also activation of the luciferase reporter in COS-7 cells that has been transfected with the cDNA containing the DRE of the rat 25(OH)D 3 -24-hydroxylase gene and cDNA of the human vitamin D nuclear receptor.
TEI-9647 can not induce cell differentiation even after treatment at 1 μM in HL-60 cell. TEI-9647 alone can not induce activation of NBT-reducing activity or α-NB esterase activity. In contrast, TEI-9647 markedly suppresses the up-regulation induced by 1α,25(OH) 2 D 3 (0.1 nM) in HL-60 cells.
TEI-9647 (0.001-1 μM; for 10 days) dose-dependently inhibits bone resorption induced by of 1α,25(OH) 2 D 3 (1 nM). TEI-9647 alone never induces bone resorption even at 1 μM.
TEI-9647 (10 nM; 12 h) markedly inhibits TAFII-17 and 25-OH-D 3 -24-hydroxylase gene expression induced by 1α,25(OH) 2 D 3 (0.1 nM) in bone marrow cells.
RT-PCR
Cell Line: HL-60 cells Concentration: 100 nM Incubation Time: 24 hours Result: Clearly suppressed p21 WAF1,CIP1 gene expression induced by 1α,25(OH) 2 D 3 .
- 更新日期:2024/08/19
- 产品编号:HY-12398
- 产品名称:(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one TEI-9647
- CAS编号:173388-20-0
- 包装:1mg
- 价格:5500元
- 更新日期:2023/10/26
- 产品编号:HY-12398
- 产品名称:(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one TEI-9647
- CAS编号:173388-20-0
- 包装:5mg
- 价格:17500元
- 公司名称:甘肃皓天科技股份有限公司
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- 公司名称:TargetMol Chemicals Inc.
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- 电子邮件:psaitong@jm-bio.com
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