2-Trifluoromethyl-2'-methoxychalcone is a Nrf2 activator. Nrf2-mediated activation of antioxidant response element is a key process of molecular mechanisms regulating the protective function of phase II detoxification and antioxidant enzymes against oxidative stress, carcinogenesis, and inflammation. In vitro: The expression of luciferase gene under the control of NQO1-ARE sequence was measured using stably transfected Beas-2B cells treated with 2-trifluoromethyl-2'-methoxychalcone. Results showed that the exposure to 2-trifluoromethyl-2'-methoxychalcone led to a significant concentration-dependent increase in luciferase activity. Moreover, Beas-2B cells were coincubated with 2-trifluoromethyl-2'-methoxychalcone and with or without N-acetylcysteine, and it was found that 2-trifluoromethyl-2'-methoxychalcone could potentially increase the expression of Nr2-regulated antioxidant genes in the presence of N-acetylcysteine . In vivo: C57BL/6 mice were treated with a single dose of vehicle or 2-trifluoromethyl-2'-methoxychalcone or sulforaphane as the positive control, and small intestines were harvested 24 h later. Results showed that the expression of GCLM and NQO1 in the small intestine of mice treated with 2-trifluoromethyl-2'-methoxychalcone was 6-fold and 10-fold higher compared to vehicle, respectively. In addition, the expression of GCLM and NQO1 in the small intestine treated with 2-trifluoromethyl-2'-methoxychalcone was 3-fold and 5-fold higher compared to sulforaphane, respectively . Clinical trial: Up to now, 2-trifluoromethyl-2'-methoxychalcone is still in the preclinical development stage.

Product information

CAS Number: 1309371-03-6

Molecular Weight: 306.28

Formula: C17H13F3O2

Chemical Name: (2E)-1-(2-methoxyphenyl)-3-[2-(trifluoromethyl)phenyl]prop-2-en-1-one

Smiles: COC1C=CC=CC=1C(=O)/C=C/C1=CC=CC=C1C(F)(F)F

InChiKey: BDZOPPCXQXPRKH-ZHACJKMWSA-N

InChi: InChI=1S/C17H13F3O2/c1-22-16-9-5-3-7-13(16)15(21)11-10-12-6-2-4-8-14(12)17(18,19)20/h2-11H,1H3/b11-10+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.