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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.
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 436.74. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.58 mL||22.9 mL||45.79 mL|
|2.5 mM||0.92 mL||4.58 mL||9.16 mL|
|5 mM||0.46 mL||2.29 mL||4.58 mL|
|25 mM||0.09 mL||0.46 mL||0.92 mL|
References are publications that support the biological activity of the product.
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 PMID: 12611900
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. 332 106 PMID: 19820207
Moreau et al (2007) Constitutive androstane receptor-vitamin D receptor crosstalk: consequence on CYP24 gene expression. Biochem.Biophys.Res.Comm. 360 76
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Keywords: CITCO, CITCO supplier, Selective, CAR, agonists, Constitutive, androstane, VDR-like, receptors, Androstane, Receptor, 3683, Tocris Bioscience
3 Citations for CITCO
Citations are publications that use Tocris products. Selected citations for CITCO include:
McMahon et al (2019) Constitutive androstane receptor 1 is constitutively bound to chromatin and 'primed' for transactivation in hepatocytes. Mol Pharmacol 95 97 PMID: 30361333
Cherian et al (2015) CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol Pharmacol 87 878 PMID: 25762023
Yueh et al (2012) Triclocarban mediates induction of xenobiotic metabolism through activation of the constitutive androstane receptor and the estrogen receptor alpha. PLoS One 7 e37705 PMID: 22761658
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