TEI-9647 |
Catalog No.GC61768
One-Click Copy Product Info
|
TEI-9647 is a vitamin D3 lactone analog that specifically inhibits vitamin D receptor activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 173388-20-0
Sample solution is provided at 25 µL, 10mM.
TEI-9647 is a vitamin D3 lactone analog that specifically inhibits vitamin D receptor activity[1-2]. TEI-9647 has anti-inflammatory effects and has also been used in research exploring the treatment of Paget's disease[3-4].
In vitro, when human promyelocytic leukemia cells (HL-60) were pretreated with TEI-9647 (1nM–1μM) for 24–96 hours, TEI-9647 significantly inhibited HL-60 cell differentiation[5].
In vivo, a single intravenous co-administration of TEI-9647 (2–50μg/kg) with 1α,25(OH)₂D₃ (0.25μg/kg) to vitamin D-deficient rats significantly suppressed the genomic effects of 1α,25(OH)₂D₃ on intestinal calcium transport and bone calcium mobilization 24 hours after treatment[6].
References:
[1] Takenouchi K, Sogawa R, Manabe K, 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.
[2] Miura D, Manabe K, Ozono K, et al. Antagonistic action of novel 1alpha,25-dihydroxyvitamin D3-26, 23-lactone analogs on differentiation of human leukemia cells (HL-60) induced by 1alpha,25-dihydroxyvitamin D3. J Biol Chem. 1999 Jun 4;274(23):16392-9.
[3] Dixon KM, Deo SS, Wong G, et al. Skin cancer prevention: a possible role of 1,25dihydroxyvitamin D3 and its analogs. J Steroid Biochem Mol Biol. 2005 Oct;97(1-2):137-43.
[4] Díaz L, Noyola-Martínez N, Barrera D, et al. Calcitriol inhibits TNF-alpha-induced inflammatory cytokines in human trophoblasts. J Reprod Immunol. 2009 Jul;81(1):17-24.
[5] Ishizuka S, Kurihara N, Hiruma Y, et al. 1alpha,25-Dihydroxyvitamin D(3)-26,23-lactam analogues function as vitamin D receptor antagonists in human and rodent cells. J Steroid Biochem Mol Biol. 2008 Jun;110(3-5):269-77.
[6] Ishizuka S, Miura D, Ozono K, et al. Antagonistic Actions in Vivo of (23S)-25-Dehydro-1alpha-Hydroxyvitamin D(3-)26,23-Lactone on Calcium Metabolism Induced by 1alpha,25-Dihydroxyvitamin D(3). Endocrinology. 2001 Jan;142(1):59-67.
| Cell experiment [1]: | |
Cell lines | HL-60 cells (human promyelocytic leukemia cell line) |
Preparation Method | HL-60 cells were cultured in RPMI-1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with TEI-9647 (1nM-1μM) for 24 hours (gene expression) or 96 hours (differentiation). |
Reaction Conditions | 1nM-1μM for 24 hours (gene expression), 96 hours (HL-60 differentiation). |
Applications | TEI-9647 significantly inhibited differentiation of HL-60 cells. |
| Animal experiment [2]: | |
Animal models | Vitamin D-deficient (-D) rats |
Preparation Method | -D rats were fed a vitamin D-deficient, low calcium diet for 7 weeks. Rats received single intravenous (iv) doses of TEI-9647 (2–50μg/kg) alone or in combination with 1α,25(OH)₂D₃ (0.25–0.5μg/kg). |
Dosage form | 2–50μg/kg; iv; Single injection. |
Applications | TEI-9647 alone weakly stimulated intestinal calcium transport and bone calcium mobilization at 8 hours but not at 24 hours in -D rats. When co-administered with 1α,25(OH)₂D₃, TEI-9647 dose-dependently antagonized 1α,25(OH)₂D₃-induced hypercalcemia, intestinal calcium absorption, and bone calcium mobilization at 24 hours. TEI-9647 also reversed 1α,25(OH)₂D₃-mediated suppression of serum PTH levels. |
References: | |
| Cas No. | 173388-20-0 | SDF | |
| Canonical 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 | ||
| Formula | C27H38O4 | M.Wt | 426.59 |
| Solubility | DMSO : 100 mg/mL (234.42 mM; Need ultrasonic) | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3442 mL | 11.7209 mL | 23.4417 mL |
| 5 mM | 468.8 μL | 2.3442 mL | 4.6883 mL |
| 10 mM | 234.4 μL | 1.1721 mL | 2.3442 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)