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- 2025年12月05日
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- 保存条件：
-20°C, protect from light, stored under nitrogen
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
173388-20-0
- 规格：
1 mg
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TEI-9647
CAS No. : 173388-20-0
MCE 国际站：TEI-9647
产品活性：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。
研究领域：Vitamin D Related/Nuclear Receptor
作用靶点：VD/VDR
In Vitro: TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21WAF1,CIP1 gene expression induced by 1α,25(OH)2D3.
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)2D3. TEI-9647 completely blocks the increase in CD11b and the decrease in CD71 expression at 100 nM.
TEI-9647 blocks both 1α,25(OH)2D3-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)D3-24-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)2D3 (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)2D3 (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-D3-24-hydroxylase gene expression induced by 1α,25(OH)2D3 (0.1 nM) in bone marrow cells.
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文献和实验Southern Hybridization Protocols
(Polyvinyl pyrrolidone) (Fisher Bioreagents) 300mg BSA (A-9647 Sigma) Top up autoclaved H2O up to 30ml (do NOT autoclave solution: BSA will coagulate!) Filter with 0.2 m . Store at -20℃ Preparation of 50% dextran sulphate (10ml) 5g Dextran sulphate 10
(Sigma A-9647) sddH2 O to 5 ml (aliquot and store at -20℃) 100 mM calcium chloride (CaCl2) : 1.48 g CaCl2-2H2 O ddH2 O to 100 ml autoclave to sterilize (store at 4deg.C).50 mM calcium chloride : 0.74 g CaCl2-2H2 O ddH2 O to 100 ml autoclave
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