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173388-20-0

中文名稱 (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
英文名稱 (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 173388-20-0
分子式 C27H38O4
分子量 426.59
MOL 文件 173388-20-0.mol
173388-20-0 結(jié)構(gòu)式 173388-20-0 結(jié)構(gòu)式

基本信息

中文別名
TEL9647
英文別名
TEL9647
TEI-9647
2(3H)-Furanone, 5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylenecyclohexylidene]ethylidene]octahydro-7a-methyl-1H-inden-1-yl]propyl]dihydro-3-methylene-, (5S)-
(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

物理化學(xué)性質(zhì)

沸點618.5±55.0 °C(Predicted)
密度1.14±0.1 g/cm3(Predicted)
儲存條件4°C, protect from light, stored under nitrogen
溶解度溶于乙醇
酸度系數(shù)(pKa)14.43±0.40(Predicted)
形態(tài)Solid
顏色White to yellow

常見問題列表

生物活性
TEI-9647 是一種 Vitamin D3 Lactone 類似物,是一種有效的,特異性的維生素 D 受體 (VDR) 拮抗劑。 TEI-9647 抑制 VDR/VDRE 介導(dǎo)的 1α,25(OH)2D3 的基因組作用。TEI-9647 可以抑制 1α,25(OH)2D3 誘導(dǎo)的骨吸收和 HL-60 細胞分化。TEI-9647 有潛力用于抑制 Paget 病中過度的骨吸收和破骨細胞形成。
體外研究

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 .
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