CITCO

• CAT Number: I006144
• CAS Number: 338404-52-7
• Molecular Formula: C19H12Cl3N3OS
• Molecular Weight: 436.73
• Purity: ≥95%
• Target: Androgen Receptor
• Solubility: Soluble in DMSO, not in water
• Storage: Store at -20C
• IUPAC Name: (E)-1-[6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]-N-[(3,4-dichlorophenyl)methoxy]methanimine
• InChI: InChI=1S/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+
• InChIKey: ZQWBOKJVVYNKTL-AUEPDCJTSA-N
• SMILES: C1=CC(=CC=C1C2=C(N3C=CSC3=N2)C=NOCC4=CC(=C(C=C4)Cl)Cl)Cl

CITCO (Cat.No:I006144) is a potent constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). CITCO altered expression of key drug-metabolizing enzymes and transporters in human hepatocytes, which positively affects the metabolic profile of CHOP. Coadministration of CITCO and CHOP in the coculture model led to significantly enhanced cytotoxicity in lymphoma cells but not in cardiomyocytes. Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss. The constitutive androstane receptor (CAR and NR1i3) is a key regulator of CYP2B6.

Reference

1:Constitutive androstane receptor upregulates Abcb1 and Abcg2 at the blood-brain barrier after CITCO activation. Lemmen J, Tozakidis IE, Bele P, Galla HJ.Brain Res. 2013 Mar 21;1501:68-80. doi: 10.1016/j.brainres.2013.01.025. Epub 2013 Jan 20. PMID: 23340159 2:Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. Chakraborty S, Kanakasabai S, Bright JJ.Br J Cancer. 2011 Feb 1;104(3):448-59. doi: 10.1038/sj.bjc.6606064. Epub 2011 Jan 11. PMID: 21224854 Free PMC Article