TEI-9647 - CAS:173388-20-0

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TEI-9647

目录号 : KM5125 CAS No. : 173388-20-0 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

TEI-9647, a Vitamin D₃ Lactone analogue, is a potent and specific vitamin 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.

体外研究

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-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.

RT-PCR

Cell Line:	HL-60 cells
Concentration:	100 nM
Incubation Time:	24 hours
Result:	Clearly suppressed p21 gene expression induced by 1α,25(OH)₂D₃.

分子式

C₂₇H₃₈O₄

分子量

426.59

CAS号

173388-20-0

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 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。