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].

TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21^WAF1,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].

426.59

Solid

C₂₇H₃₈O₄

173388-20-0

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

DMSO : 100 mg/mL(234.42 mM;Need ultrasonic)

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。

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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 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。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 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。