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Description: Selective CAR agonist
Chemical Name: 6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl)oxime
Purity: ≥98% (HPLC)
Biological Activity for CITCO
CITCO is a 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.
Compound Libraries for CITCO
CITCO is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CITCO
| M. Wt | 436.74 |
| Formula | C19H12Cl3N3OS |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 338404-52-7 |
| PubChem ID | 9600409 |
| InChI Key | ZQWBOKJVVYNKTL-AUEPDCJTSA-N |
| Smiles | ClC(C(Cl)=C4)=CC=C4CO/N=C/C1=C(C3=CC=C(Cl)C=C3)N=C2N1C=CS2 |
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.
Solubility Data for CITCO
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.84 | 50 |
Preparing Stock Solutions for CITCO
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 |
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Product Datasheets for CITCO
References for CITCO
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 PMID: 17585873
If you know of a relevant reference for CITCO, please let us know.
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Keywords: CITCO, CITCO supplier, Selective, CAR, agonists, Constitutive, androstane, VDR-like, receptors, Androstane, Receptor, 3683, Tocris Bioscience
4 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
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
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
Petr et al (2021) (E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells. Front Pharmacol 12 713149 PMID: 34483922
Do you know of a great paper that uses CITCO from Tocris? Please let us know.
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