1383816-33-8

Basic information

• Product Name: 2-(3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-methoxybenzo[d]thiazole-6-carboxylic acid
• Synonyms: 2-(3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-methoxybenzo[d]thiazole-6-carboxylic acid
• CAS NO: 1383816-33-8
• Molecular Weight: 615.63
• Mol File: 1383816-33-8.mol
• Article Data: 2

Chemical Properties

• CAS DataBase Reference: 2-(3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-methoxybenzo[d]thiazole-6-carboxylic acid(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-methoxybenzo[d]thiazole-6-carboxylic acid(1383816-33-8)
• EPA Substance Registry System: 2-(3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-methoxybenzo[d]thiazole-6-carboxylic acid(1383816-33-8)

Safety Data

• Hazardous Substances Data: 1383816-33-8(Hazardous Substances Data)

Upstream product

• 543713-03-7 N-hydroxy-2-(trifluoromethoxy)benzimidonyl chloride 
• 1383740-05-3 methyl 2-chloro-4-methoxy-1,3-benzothiazole-6-carboxylate 
• 1383822-31-8 (1R,3S,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octane 
• 1383816-32-7 methyl 2-(3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-methoxybenzo[d]thiazole-6-carboxylate 
• 1383740-01-9 (Z)-N-hydroxy-2-(trifluoromethoxy)benzimidoyl chloride 
• 1383740-00-8 (E)-2-(trifluoromethoxy)benzaldehyde oxime 
• 1103500-32-8 methyl 5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazole-4-carboxylate 
• 955886-84-7 methyl 2-amino-4-methoxy-1,3-benzothiazole-6-carboxylate 
• 946427-86-7 4-(bromomethyl)-5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazole 
• 41608-64-4 methyl 3-methoxy-4-aminobenzoate 
• 94651-33-9 2-(trifluoromethoxy)benzaldehyde 

Relevant articles and documents

Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)

The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases bile acid conjugation, transport, and excretion, thereby protecting the liver from the harmful effects of bile accumulation, leading to considerable interest in FXR as a therapeutic target for the treatment of cholestasis and nonalcoholic steatohepatitis. We identified a novel series of highly potent non-bile acid FXR agonists that introduce a bicyclic nortropine-substituted benzothiazole carboxylic acid moiety onto a trisubstituted isoxazole scaffold. Herein, we report the discovery of 1 (tropifexor, LJN452), a novel and highly potent agonist of FXR. Potent in vivo activity was demonstrated in rodent PD models by measuring the induction of FXR target genes in various tissues. Tropifexor has advanced into phase 2 human clinical trials in patients with NASH and PBC.