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CITCO

Cat No. 3683

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Chemical Name: 6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbald ehyde-O-(3,4-dichlorobenzyl)oxime

Biological Activity

Constitutive androstane receptor (CAR) agonist (EC₅₀ = 49 nM). Displays > 100-fold selectivity over PXR receptors and no activity at LXR, ERα, ERβ, PPAR, RAR, FXR, VDR and THR. Induces CAR nuclear translocation and expression of CYP2B6 in hepatocytes in vitro.

Technical Data

M.Wt:

436.74

Formula:

C₁₉H₁₂Cl₃N₃OS

Solubility:

Soluble to 50 mM in DMSO and to 5 mM in ethanol

Purity:

>98 %

Storage:

Desiccate at -20°C

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

Maglich et al (2003) Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. J.Biol.Chem. 278 17277. Moreau et al (2007) Constitutive androstane receptor-vitamin D receptor crosstalk: consequence on CYP24 gene expression. Biochem.Biophys.Res.Comm. 360 76. Clen et al (2009) A single amino acid controls the functional switch of human CAR1 to the xenobiotic sensitive splicing variant CAR3. J.Pharmacol.Exp.Ther. (in press)

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