1227612-52-3

Upstream product

• 1711-10-0 3-iodobenzoyl chloride 
• 1227612-51-2 methyl 3α-acetoxy-7α-hydroxy-6α-ethyl-5β-cholan-24-oate 
• 618-51-9 3-Iodobenzoic acid 
• 951694-73-8 methyl (4R)-4-((3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoate 

Downstream Products

• 1359697-61-2 methyl 6α-ethyl-7α-(3'-iodobenozyl)oxy-3,16-dihydroxy-5β-cholan-24-oate 
• 1359697-59-8 3α,16α,24-trihydroxy-6α-ethyl-7α-(3'-iodobenozyl)oxy-5β-cholane 
• 1227612-54-5 methyl Δ16-3α-acetoxy-6α-ethyl-7α-(3'-iodobenozyl)oxy-5β-cholan-24-oate 

Relevant academic research and scientific papers

Avicholic acid: A lead compound from birds on the route to potent TGR5 modulators

Grounding on our former 3D QSAR studies, a knowledge-based screen of natural bile acids from diverse animal species has led to the identification of avicholic acid as a selective but weak TGR5 agonist. Chemical modifications of this compound resulted in the disclosure of 6α-ethyl-16-epi-avicholic acid that shows enhanced potency at TGR5 and FXR receptors. The synthesis, biological appraisals, and structure-activity relationships of this series of compounds are herein described. Moreover, a thorough physicochemical characterization of 6α-ethyl-16-epi-avicholic acid as compared to naturally occurring bile acids is reported and discussed.

TGR5 MODULATORS AND METHODS OF USE THEREOF

The invention relates to compounds of Formula (A): (A) or a salt, solvate, hydrate, or amino acid conjugate thereof. The compounds of formula A are TGR5 modulators useful for the prevention and treatment of disease.