TEI-9647

Cat. No.: HY-12398: FAQs
Data Sheet SDS Handling Instructions

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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.

For research use only. We do not sell to patients.

TEI-9647 Chemical Structure

CAS No. : 173388-20-0

Size	Price	Stock
1 mg	USD 550	Ask For Quote & Lead Time
5 mg	USD 1750	Ask For Quote & Lead Time
10 mg	USD 2850	Ask For Quote & Lead Time

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Other Forms of TEI-9647:

TEI-9648 In-stock

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21^WAF1,CIP1 gene 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[1]

Cell Line:	HL-60 cells
Concentration:	100 nM
Incubation Time:	24 hours
Result:	Clearly suppressed p21^WAF1,CIP1 gene expression induced by 1α,25(OH)₂D₃.

Molecular Weight

426.59

Formula

C₂₇H₃₈O₄

CAS No.

173388-20-0

Appearance

Solid

Color

White to yellow

SMILES

O=C1O[C@@H](C[C@H]([C@H]2CC[C@@]3([H])/C(CCC[C@]23C)=C/C=C4C([C@@H](O)C[C@H](O)C\4)=C)C)CC1=C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (234.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Data Sheet (276 KB) SDS (252 KB) Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[3]. Kazuya Takenouchi, et al. Synthesis and structure-activity relationships of TEI-9647 derivatives as Vitamin D₃ antagonists. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):31-4. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3442 mL	11.7209 mL	23.4417 mL	58.6043 mL
	5 mM	0.4688 mL	2.3442 mL	4.6883 mL	11.7209 mL
	10 mM	0.2344 mL	1.1721 mL	2.3442 mL	5.8604 mL
	15 mM	0.1563 mL	0.7814 mL	1.5628 mL	3.9070 mL
	20 mM	0.1172 mL	0.5860 mL	1.1721 mL	2.9302 mL
	25 mM	0.0938 mL	0.4688 mL	0.9377 mL	2.3442 mL
	30 mM	0.0781 mL	0.3907 mL	0.7814 mL	1.9535 mL
	40 mM	0.0586 mL	0.2930 mL	0.5860 mL	1.4651 mL
	50 mM	0.0469 mL	0.2344 mL	0.4688 mL	1.1721 mL
	60 mM	0.0391 mL	0.1953 mL	0.3907 mL	0.9767 mL
	80 mM	0.0293 mL	0.1465 mL	0.2930 mL	0.7326 mL
	100 mM	0.0234 mL	0.1172 mL	0.2344 mL	0.5860 mL

TEI-9647 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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