Product Name :
TEI-9647
Description:
TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget’s disease.
CAS:
173388-20-0
Molecular Weight:
426.59
Formula:
C27H38O4
Chemical Name:
(5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-{2-[(1Z,3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene}-7a-methyl-octahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one
Smiles :
C[C@H](C[C@H]1CC(=C)C(=O)O1)[C@H]1CC[C@H]2/C(/CCC[C@@]21C)=C/C=C1/C[C@@H](O)C[C@H](O)C/1=C
InChiKey:
SAODSJHDCZTVAT-CZADFQNYSA-N
InChi :
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
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget’s disease.|Product information|CAS Number: 173388-20-0|Molecular Weight: 426.59|Formula: C27H38O4|Chemical Name: (5S)-5-[(2R)-2-[(1R,3aS,4E,7aR)-4-{2-[(1Z,3S,5R)-3,5-dihydroxy-2-methylidenecyclohexylidene]ethylidene}-7a-methyl-octahydro-1H-inden-1-yl]propyl]-3-methylideneoxolan-2-one|Smiles: C[C@H](C[C@H]1CC(=C)C(=O)O1)[C@H]1CC[C@H]2/C(/CCC[C@@]21C)=C/C=C1/C[C@@H](O)C[C@H](O)C/1=C|InChiKey: SAODSJHDCZTVAT-CZADFQNYSA-N|InChi: 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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 100 mg/mL (234.42 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|TEI-9647 (100 nM; 24 hours) treatment clearly suppresses p21WAF1,CIP1 gene expression induced by 1α,25(OH)2D3. TEI-9647 (10-1000 nM; 96 hours) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH)2D3.{{Tecovirimat} web|{Tecovirimat} Anti-infection|{Tecovirimat} Biological Activity|{Tecovirimat} In Vitro|{Tecovirimat} custom synthesis|{Tecovirimat} Epigenetics} TEI-9647 completely blocks the increase in CD11b and the decrease in CD71 expression at 100 nM.{{Hydroxyethyl cellulose} site|{Hydroxyethyl cellulose} {Biochemical Assay Reagents}|{Hydroxyethyl cellulose} Protocol|{Hydroxyethyl cellulose} Data Sheet|{Hydroxyethyl cellulose} manufacturer|{Hydroxyethyl cellulose} Epigenetic Reader Domain} TEI-9647 blocks both 1α,25(OH)2D3-mediated HL-60 cell differentiation and also activation of the luciferase reporter in COS-7 cells that has been transfected with the cDNA containing the DRE of the rat 25(OH)D3-24-hydroxylase gene and cDNA of the human vitamin D nuclear receptor.PMID:23381601 TEI-9647 can not induce cell differentiation even after treatment at 1 μM in HL-60 cell. TEI-9647 alone can not induce activation of NBT-reducing activity or α-NB esterase activity. In contrast, TEI-9647 markedly suppresses the up-regulation induced by 1α,25(OH)2D3 (0.1 nM) in HL-60 cells. TEI-9647 (0.001-1 μM; for 10 days) dose-dependently inhibits bone resorption induced by of 1α,25(OH)2D3 (1 nM). TEI-9647 alone never induces bone resorption even at 1 μM. TEI-9647 (10 nM; 12 h) markedly inhibits TAFII-17 and 25-OH-D3-24-hydroxylase gene expression induced by 1α,25(OH)2D3 (0.1 nM) in bone marrow cells.|Products are for research use only. Not for human use.|