| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
TEI-9648 is a specific antagonist of the Vitamin D Receptor (VDR). It functions by binding to the VDR and blocking its ability to interact with the Vitamin D Response Element (VDRE) on DNA, thereby inhibiting the genomic actions of the active vitamin D hormone 1alpha,25(OH)2D3.
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| ln Vitro |
TEI-9648 (10-1000 nM) inhibits the reciprocal changes in CD11b and CD71 expression linked to 1α,25(OH)2D3-induced HL-60 cell differentiation in a dose-dependent manner[1]. Compared to TEI-9647, TEI-9648 consistently exhibits a weaker suppressing effect[1]. Even after treating HL-60 cells at a concentration of 1 μM, TEI-9648 is unable to stimulate cell differentiation[1]. NBT-reducing activity and α-NB esterase activity cannot be activated by TEI-9648 alone. On the other hand, TEI-9648 significantly reduces the up-regulation in HL-60 cells caused by 1α,25(OH)2D3 (0.1 nM)[1].
TEI-9648 is a potent and specific VDR antagonist. It effectively blocks 1alpha,25(OH)2D3-induced actions, including gene transcription and cell differentiation. It does not induce cell differentiation in HL-60 leukemia cells even at high concentrations (1 microM), but it potently suppresses the differentiation that would normally be induced by 1alpha,25(OH)2D3. |
| ln Vivo |
TEI-9648 is used in vivo to study the role of VDR and vitamin D in biological processes. By blocking VDR, it serves as a tool to dissect which effects of vitamin D are mediated through its receptor versus non-genomic pathways, particularly in studies of bone metabolism and cellular differentiation.
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| Enzyme Assay |
Cell-free VDR binding assays are performed by incubating the VDR receptor with a radiolabeled form of 1alpha,25(OH)2D3 and varying concentrations of TEI-9648. After incubation to reach equilibrium, bound and free ligands are separated, and the half-maximal inhibitory concentration (IC50) is determined via scintillation counting.
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| Cell Assay |
Cellular assays are performed using HL-60 human promyelocytic leukemia cells, which differentiate along the monocytic/macrophage lineage upon treatment with 1alpha,25(OH)2D3. TEI-9648 is added to the culture with or without 1alpha,25(OH)2D3. Cell differentiation is measured by the expression of surface markers CD11b and CD71 using flow cytometry or by assessing NBT (nitroblue tetrazolium) reducing activity.
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| Animal Protocol |
In vivo data is not available for this research compound. As a laboratory chemical for cell-based and in vitro studies, it is not typically formulated for animal pharmacokinetic or efficacy studies in a standard research setting.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties are not documented. As a laboratory chemical primarily for in vitro use, ADME (Absorption, Distribution, Metabolism, Excretion) data are not typically required or reported.
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| Toxicity/Toxicokinetics |
Toxicological and safety profiles have not been formally established. This compound is intended for research use only and is not for human consumption. Standard safety precautions for handling fine chemicals should be followed.
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| References |
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| Additional Infomation |
(23R)-1α-hydroxy-25,27-disehydrovitamin D3 26,23-lactone is a type of vitamin D.
TEI-9648 is a specific VDR antagonist, which makes it an invaluable tool for studying the role of the vitamin D receptor in genomic signaling. Unlike general inhibitors, its high specificity allows researchers to isolate VDR-mediated effects from other downstream pathways. It is particularly useful for bone metabolism and cancer differentiation research. It is for research use only. |
| Molecular Formula |
C27H38O4
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|---|---|
| Molecular Weight |
426.59
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| Exact Mass |
426.277
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| CAS # |
173388-21-1
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| Related CAS # |
TEI-9647;173388-20-0
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| PubChem CID |
9547693
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| Appearance |
Off-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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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
821
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@H](C[C@@H]1CC(=C)C(=O)O1)[C@H]2CC[C@@H]\3[C@@]2(CCC/C3=C\C=C/4\C[C@H](C[C@@H](C4=C)O)O)C
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| InChi Key |
SAODSJHDCZTVAT-JXJLEVNFSA-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 |
(5R)-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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| 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: 50 mg/mL (117.21 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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