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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
TEI-9647 (TEI9647) is a vitamin D receptor (VDR) antagonist with immunomodulatory effects. It prevents the production of osteoclasts from pagetic bone marrow cells that are brought on by 1,25-dihydroxyvitamin D3.
ln Vitro |
TEI-9647 (100 nM; 24 hours) treatment distinctly reduces the expression of the p21WAF1,CIP1 gene that is triggered by 1α,25(OH)2D3[1].
TEI-9647 (10-1000 nM; 96 hours) blocks in a dose-dependent manner the reciprocal changes in CD11b and CD71 expression linked to 1α,25(OH)2D3-induced HL-60 cell differentiation. At 100 nM, TEI-9647 totally inhibits both the rise in CD11b and the fall in CD71 expression[1]. TEI-9647 blocks the luciferase reporter's activation in COS-7 cells transfected with the human vitamin D nuclear receptor and rat 25(OH)D3-24-hydroxylase gene's DRE, as well as 1α,25(OH)2D3-mediated HL-60 cell differentiation[1]. TEI-9647 cannot bring about cell differentiation in HL-60 cells, not even after treatment at 1 μM. TEI-9647 is unable to activate α-NB esterase or NBT-reducing activity on its own. On the other hand, 1α,25(OH)2D3 (0.1 nM)-induced up-regulation in HL-60 cells is significantly suppressed by TEI-9647[1]. TEI-9647 (0.001-1 μM; for 10 days) inhibits bone resorption caused by 1α,25(OH)2D3 (1 nM) in a dose-dependent manner. Even at 1 μM, TEI-9647 by itself never causes bone resorption[2]. TEI-9647 (10 nM; 12 h) significantly reduces the expression of the genes TAFII-17 and 25-OH-D3-24-hydroxylase that are brought on in bone marrow cells by 1α,25(OH)2D3 (0.1 nM)[2]. |
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References |
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Molecular Formula |
C27H38O4
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Molecular Weight |
426.5882
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Exact Mass |
426.277
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Elemental Analysis |
C, 76.02; H, 8.98; O, 15.00
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CAS # |
173388-20-0
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Related CAS # |
TEI-9648;173388-21-1
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Appearance |
White to yellow solid powder
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Boiling Point |
618.492ºC at 760 mmHg
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Flash Point |
204.543ºC
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Vapour Pressure |
0mmHg at 25°C
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Index of Refraction |
1.567
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LogP |
5.025
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SMILES |
O1C(C(=C([H])[H])C([H])([H])[C@]1([H])C([H])([H])[C@@]([H])(C([H])([H])[H])[C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])/C(=C(\[H])/C(/[H])=C3\C(=C([H])[H])[C@]([H])(C([H])([H])[C@@]([H])(C\3([H])[H])O[H])O[H])/C([H])([H])C([H])([H])C([H])([H])[C@]12C([H])([H])[H])=O
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InChi Key |
SAODSJHDCZTVAT-CZADFQNYSA-N
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InChi Code |
InChI=1S/C27H38O4/c1-16(12-22-13-17(2)26(30)31-22)23-9-10-24-19(6-5-11-27(23,24)4)7-8-20-14-21(28)15-25(29)18(20)3/h7-8,16,21-25,28-29H,2-3,5-6,9-15H2,1,4H3/b19-7+,20-8-/t16-,21-,22+,23-,24+,25+,27-/m1/s1
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Chemical Name |
(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-[(2Z)-2-[(3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one
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Synonyms |
TEI 9647; TEI9647; TEI-9647
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~234.4 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.86 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.86 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.86 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Antagonistic action of TEI-9647 on 1α,25(OH)2D3( VDR )-mediated expression of the 25(OH)D3-24-hydroxylase gene in a luciferase reporter assay. J Biol Chem . 1999 Jun 4;274(23):16392-9. td> |
Effects of TEI-9647 on 1α,25(OH)2D3-induced HL-60 cell differentiation as examined with cell surface marker expression. J Biol Chem . 1999 Jun 4;274(23):16392-9. td> |
Effects of TEI-9647 and TEI-9648 on KH-1060-induced HL-60 cell differentiation. J Biol Chem . 1999 Jun 4;274(23):16392-9. td> |
Effects of TEI-9647 and TEI-9648 on 1α,25(OH)2D3-induced HL-60 cell differentiation as examined with NBT-reducing activity. J Biol Chem . 1999 Jun 4;274(23):16392-9. td> |