338404-52-7

CITCO has been used for the activation of mouse constitutive androstane receptor (CAR) and human CAR.

ChEBI: 1-[6-(4-chlorophenyl)-5-imidazo[2,1-b]thiazolyl]-N-[(3,4-dichlorophenyl)methoxy]methanimine is a member of imidazoles.

CITCO is an imidazothiazole derivative. It stimulates human constitutive androstane receptor (CAR) nuclear translocation.

citco, an imidazothiazole derivative, is a selective agonist of human car, with an ec50 value of 49 nm and > 50-fold selectivity to car over pregnane x receptor (pxr), and no activity on other nuclear receptors. upon activation with specific agonists, car translocates into the nucleus and binds to the response elements as monomers or car/rxr heterodimers. the car functions as a xenobiotic receptor, involved in detoxification and clearance of toxic substances from the liver. in addition, activation with selective car agonists such as citco has also been shown to inhibit growth and expansion of brain tumor stem cells.1. chakraborty s, kanakasabai s, bright jj. constitutive androstane receptor agonist citco inhibits growth and expansion of brain tumour stem cells. british journal of cancer, 2011, 104(3): 448-459.

CITCO is a constitutive androstane receptor (CAR) agonist; nuclear receptor NR113 agonist.

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