338404-52-7 Usage
Description
CITCO, an imidazothiazole derivative, is a compound that plays a significant role in the activation and stimulation of the mouse constitutive androstane receptor (CAR) and human CAR. This activation leads to the nuclear translocation of the receptor, which is crucial for various cellular processes and functions.
Uses
Used in Pharmaceutical Industry:
CITCO is used as an activator for the mouse constitutive androstane receptor (CAR) and human CAR. This activation is essential for the proper functioning of these receptors, which play a vital role in the regulation of various cellular processes, including metabolism, detoxification, and cellular signaling.
Used in Research and Development:
CITCO is also utilized in research and development for studying the role of CAR in various biological processes and its potential therapeutic applications. By activating and stimulating CAR, researchers can gain insights into the receptor's function and its potential role in the development of new drugs and therapies.
Used in Drug Discovery:
CITCO's ability to activate CAR makes it a valuable tool in drug discovery, as it can be used to identify potential drug candidates that target this receptor. This can lead to the development of new treatments for various diseases and conditions, particularly those related to metabolism and detoxification.
Biological Activity
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.
Biochem/physiol Actions
CITCO is a constitutive androstane receptor (CAR) agonist; nuclear receptor NR113 agonist.
Check Digit Verification of cas no
The CAS Registry Mumber 338404-52-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,3,8,4,0 and 4 respectively; the second part has 2 digits, 5 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 338404-52:
(8*3)+(7*3)+(6*8)+(5*4)+(4*0)+(3*4)+(2*5)+(1*2)=137
137 % 10 = 7
So 338404-52-7 is a valid CAS Registry Number.
InChI:InChI=1/C19H12Cl3N3OS/c20-14-4-2-13(3-5-14)18-17(25-7-8-27-19(25)24-18)10-23-26-11-12-1-6-15(21)16(22)9-12/h1-10H,11H2/b23-10+
338404-52-7Relevant articles and documents
Stereoisomerization of human constitutive androstane receptor agonist CITCO
Deschamps, Jeffrey R.,Diethelm-Varela, Benjamin,Imler, Gregory H.,Kumar, Anmol,Li, Yue,Lynch, Caitlin,MacKerell, Alexander D.,Xia, Menghang,Xue, Fengtian
supporting information, (2020/12/25)
CITCO (6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl) oxime) is a widely used agonist of the human constitutive androstane receptor (hCAR), a key hepatic xenobiotic sensor protein with emerging therapeutic indications.
CAR ACTIVATOR AGENTS FOR CYCLOPHOSPHAMIDE-BASED TREATMENTS OF CANCER
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Page/Page column 84; 85; 87, (2019/01/10)
The invention relates to selective small molecule human constitutive androstane receptor (hCAR) activators of Formula (I) or (II), pharmaceutical compositions thereof, and use thereof for the treatment of hematologic malignancies and other cancers. The sm
