Bile Acid-Gut Microbiome Axis The microbiome plays a major role in the biotransformation of nutrients and xenobiotics in the body, which can alter the pharmacology and/or toxicology of these chemicals. A clear example of this is how intestinal microbiota transform bile acids, which act as modulators at bile acid receptors (FXR and TGR5) to affect signaling pathways related to bile acid synthesis and energy metabolism regulation. Cayman offers a wide range of primary and secondary bile acids as well as cell-based assays for easy assessment of potential modulators of FXR and TGR5. Fat Muscle Liver TGR5 TGR5 1° Bile Acid ynthesis Stomach Large Intestine TGR5 Bile acids FXR Primary TGR5 L cells bile acids GP-1 Common Secondary bile duct bile acids Small Intestine Bile acids 2° Bile Acid ynthesis Portal vein Duodenum FXR Ileocytes FXR FXR FGF151 Bile Acids, Conjugates, and Metabolites Item No. Product Name Item No. Product Name 10011286 Chenodeoxycholic Acid* 20293 Hyocholic Acid 20250 Cholic Acid* 20294 Hyodeoxycholic Acid 9002532 Cholic Acid 7-sulfate 20253 Lithocholic Acid* 20756 Deoxycholic Acid* 20676 Lithocholic Acid 3-sulfate (sodium salt) 16942 Glycochenodeoxycholic Acid (sodium salt hydrate)* 20291 α-Muricholic Acid 20276 Glycocholic Acid* 20288 Tauro-α-muricholic Acid (sodium salt) 20274 Glycodeoxycholic Acid (hydrate) 20287 β-Muricholic Acid 22670 Glycohyocholic Acid 9003230 Glycine-β-muricholic Acid 22643 Glycohyodeoxycholic Acid 20289 Tauro-β-muricholic Acid (sodium salt) 21723 Glycolithocholic Acid 20292 ω-Muricholic Acid 21698 Glycoursodeoxycholic Acid 20290 Murideoxycholic Acid *Also available: isotopically labeled internal standards 2020 CAYMAN CHEMICAL · 1180 EAST ELLSWORTH ROAD · ANN ARBOR, MI 48108 · USA · (800) 364-9897 WWW.CAYMANCHEM.COM Bile Acids, Conjugates, and Metabolites (continued) Item No. Product Name Item No. Product Name 20275 Taurochenodeoxycholic Acid (sodium salt)* 21956 Taurohyodeoxycholic Acid 16215 Taurocholic Acid (sodium salt)* 17275 Taurolithocholic Acid (sodium salt) 9002538 Taurocholic Acid 3-sulfate 18468 Taurolithocholic Acid 3-sulfate (sodium salt) 15935 Taurodeoxycholic Acid (sodium salt) 20277 Tauroursodeoxycholic Acid 22669 Taurohyocholic Acid 15121 Ursodeoxycholic Acid (sodium salt)* *Also available: isotopically labeled internal standards Cell-Based Assays for Evaluating Modulators of Bile Acid Receptors TGR5 (GP-BAR1) Bile Acid Nuclear Receptor FXR (NR1H4) Reporter Assay Kit Reporter Assay Kit Item No. 601440 Item No. 601790 120 120 XL335XL335 100 100 TGR5TGR5 Agonis Agonist t e e LithocholicLithocholic Acid Acid 100 100 GW 4064GW 4064 BetulinicBetulinic Acid Acid Tropifexor 80 80 Tropifexor UrsolicUrsolic Acid Acid 80 80 CDCACDCA OleanolicOleanolic Acid Acid INT-777 60 60 INT-777 60 60 DeoxycholicDeoxycholic Acid Acid CDCACDCA 40 40 40 40 20 20 20 20 % of Maximal Control Response % of Maximal Control Response % of Maximal Control Respons % of Maximal Control Respons 0 0 0 0 -9 -9 -8 -8 -7 -7 -6 -6 -5 -5 -4 -4 -12 -12-11 -11-10 -10-9 -9-8 -8-7 -7-6 -6-5 -5-4 -4 Log[Agonist], M Log[Agonist], M Log[Agonist],Log[Agonist], M M Validation of TGR5 reporter assay with different classes of agonists. Validation of FXR reporter assay with different classes of agonists. About Reverse Transfection Technology Cayman's TGR5 and FXR reporter assay kits use plates pre-coated with optimized transfection complexes, offering up to 3-fold increased transfection and >95% co-transfection efficiency (compared to traditional transfection methods) for well-to-well consistency. · No need to develop, maintain, or expand stable cell lines · Avoid cell lineage variability · Sufficient reagent provided to sample at multiple time points T 1 T 2 T 3 late cells roen cells can press Assay recover transect overnit proteins net day 10 80 60 simply test 4 add cells 20 0 1 1 1, GFP DNA Transfection >95% Co-Transfection Complex re-Coated View All Bile Acid & Microbiome products at www.caymanchem.com 2020 CAYMAN CHEMICAL · 1180 EAST ELLSWORTH ROAD · ANN ARBOR, MI 48108 · USA · (800) 364-9897 WWW.CAYMANCHEM.COM.