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Submit ReviewCITCO
说明： Selective CAR agonist
化学名： 6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl)oxime
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for CITCO
CITCO is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for CITCO
| 分子量 | 436.74 |
| 公式 | C19H12Cl3N3OS |
| 储存 | Desiccate at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CITCO
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 21.84 | 50 |
制备储备液 for CITCO
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for CITCO
参考文献 for CITCO
参考文献是支持产品生物活性的出版物。
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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关键词: CITCO, CITCO supplier, Selective, CAR, agonists, Constitutive, androstane, VDR-like, receptors, Androstane, Receptor, 3683, Tocris Bioscience
4 篇 CITCO 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CITCO 的部分引用包括：
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
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