| Description | TEI-9648, an analogue of Vitamin D3 Lactone, acts as a potent and specific antagonist to the vitamin D receptor (VDR). This compound effectively blocks the genomic actions mediated by VDR and the Vitamin D responsive element (VDRE) of 1α,25(OH)2D3. Furthermore, TEI-9648 prevents the differentiation of HL-60 cells induced by 1α,25(OH)2D3, indicating its utility in bone metabolism studies[1][2]. |
| In vitro | TEI-9648 (10-1000 nM) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH)2D3[1]. TEI-9648 has consistently weaker suppressive effect than TEI-9647[1]. TEI-9648 can not induce cell differentiation even after treatment at 1 μM in HL-60 cell[1]. TEI-9648 alone can not induce activation of NBT-reducing activity or α-NB esterase activity. In contrast, TEI-9648 markedly suppresses the up-regulation induced by 1α,25(OH)2D3 (0.1 nM) in HL-60 cells[1]. |
| molecular weight | 426.597 |
| Molecular formula | C27H38O4 |
| CAS | 173388-21-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 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. 2. 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. |