TEI-9647 是一种 Vitamin D3Lactone 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 D3Lactone analogue, is a potent and specificvitamin D receptor (VDR)antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget's disease[1][2][3]. |
体外研究 (In Vitro) | TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21WAF1,CIP1gene expression induced by 1α,25(OH)2D3[1]. 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[1]. 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[1]. 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[1]. 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[2]. 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[2].
RT-PCR[1] Cell Line: | HL-60 cells | Concentration: | 100 nM | Incubation Time: | 24 hours | Result: | Clearly suppressed p21WAF1,CIP1gene expression induced by 1α,25(OH)2D3. |
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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) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(234.42 mM;Need ultrasonic) 配制储备液 1 mM | 2.3442 mL | 11.7209 mL | 23.4417 mL | 5 mM | 0.4688 mL | 2.3442 mL | 4.6883 mL | 10 mM | 0.2344 mL | 1.1721 mL | 2.3442 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.86 mM) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.86 mM) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.86 mM) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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