1609564-58-0

Basic information

• Product Name: (E)-2-(2-(1-(p-tolyl)ethylidene)hydrazinyl)benzo[d]thiazole
• Synonyms: (E)-2-(2-(1-(p-tolyl)ethylidene)hydrazinyl)benzo[d]thiazole
• CAS NO: 1609564-58-0
• Molecular Weight: 281.381
• Mol File: 1609564-58-0.mol

Chemical Properties

• CAS DataBase Reference: (E)-2-(2-(1-(p-tolyl)ethylidene)hydrazinyl)benzo[d]thiazole(CAS DataBase Reference)
• NIST Chemistry Reference: (E)-2-(2-(1-(p-tolyl)ethylidene)hydrazinyl)benzo[d]thiazole(1609564-58-0)
• EPA Substance Registry System: (E)-2-(2-(1-(p-tolyl)ethylidene)hydrazinyl)benzo[d]thiazole(1609564-58-0)

Safety Data

• Hazardous Substances Data: 1609564-58-0(Hazardous Substances Data)

Upstream product

• 615-21-4 1,3-benzothiazol-2-ylhydrazine 
• 122-00-9 para-methylacetophenone 

Downstream Products

• 1609564-61-5 1-(1,3-benzothiazol-2-yl)-3-(4-methylphenyl)-1H-pyrazole-4-carbaldehyde 
• 1609564-70-6 1-(benzo[d]thiazol-2-yl)-N-(4-methyl-3-(morpholinosulfonyl)phenyl)-3-(p-tolyl)-1H-pyrazole-4-carboxamide 
• 1609564-65-9 1-(benzo[d]thiazol-2-yl)-3-(p-tolyl)-1H-pyrazole-4-carboxylic acid 

Relevant articles and documents

FARNESOID X RECEPTOR ANTAGONISTS

Provided herein are Farnesoid X receptor (FXR) antagonists, methods of antagonizing FXR, and methods of treating metabolic disease using the antagonists herein.

Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor

Farnesoid X receptor (FXR, NRIH4) plays a major role in the control of cholesterol metabolism. This suggests that antagonizing the transcriptional activity of FXR is a potential means to treat cholestasis and related metabolic disorders. Here we describe the synthesis, biological evaluation, and structure-activity relationship (SAR) studies of trisubstituted-pyrazol carboxamides as novel and potent FXR antagonists. One of these novel FXR antagonists, 4j has an IC50 of 7.5 nM in an FXR binding assay and 468.5 nM in a cell-based FXR antagonistic assay. Compound 4j has no detectable FXR agonistic activity or cytotoxicity. Notably, 4j is the most potent FXR antagonist identified to date; it has a promising in vitro profile and could serve as an excellent chemical tool to elucidate the biological function of FXR.