GLPBio

TEI-9647

Catalog No.: GC61768Purity:>98.00%
COASDSData Sheet
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.

TEI-9647
Cas No.: 173388-20-0
1 mgIn Stock
$495.00
1
5 mgIn Stock
$1,575.00
1
10 mgIn Stock
$2,565.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

1 publicationsPublications from researchers using this product

Description

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.

Protocol

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:
[1] 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.
[2] 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
173388-20-0
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
Molecular Formula
C27H38O4
Molecular Weight
426.59
Solubility
DMSO : 100 mg/mL (234.42 mM; Need ultrasonic)
Storage
4°C, protect from light, stored under nitrogen
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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