TEI-9647
目录号: PL12559 纯度: ≥98%
CAS No. :173388-20-0
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中文名称
TEI-9647
中文别名
(1S,3R,5Z,7E,23S)-1,3-Dihydroxy-23,26-epoxy-9,10-secocholesta-5,7 ,10,25(27)-tetraen-26-one
英文名称
TEI-9647
英文别名
(1s,3r,5z,7e,23s)-1,3-dihydroxy-23,26-epoxy-9,10-secocholesta-5,7 ,10,25(27)-tetraen-26-one;(1S,3R,5Z;2(3H)-Fur;(1S,3R,5Z; 2(3H)-Fur;(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;TEI9647;LMST03020599;GTPL2788;BDBM50411169;Q27088957;(23S)-1-hydrox;(23S)-1alpha-Hydroxy-25,27-didehydrovitamin D3 26,23-lactone;TEI-9647
Cas No.
173388-20-0
分子式
C27H38O4
分子量
426.59
包装储存
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
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。
生物活性
TEI-9647, a Vitamin D 3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH) 2 D 3 . TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH) 2 D 3 . TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Pagets disease.
性状
Solid
体外研究(In Vitro)
TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21 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-reducin
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Miura D, et al. Antagonistic action of novel 1α,25-dihydroxyvitamin D3-26, 23-lactone analogs on differentiation of human leukemia cells (HL-60) induced by 1α,25-dihydroxyvitamin D3. J Biol Chem. 1999 Jun 4;274(23):16392-9.
[2]. Seiichi Ishizuka, et al. Vitamin D antagonist, TEI-9647, inhibits osteoclast formation induced by 1α,25-dihydroxyvitamin D3 from pagetic bone marrow cells. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):331-4.
溶解度数据
In Vitro: DMSO : 100 mg/mL (234.42 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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