A competitive antagonist of FXR (IC50 = 15 µM ) that inhibits chenodeoxycholic acid (CDCA)-induced transactivation of FXR; lowers LDL cholesterol and triglyceride levels in rodents fed a high cholesterol diet

(E)-Guggulsterone – 1 mg

Brand:
Cayman
CAS:
39025-24-6
Storage:
-20
UN-No:
Non-Hazardous - /

Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.{10943} They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.{14024,16793} Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hyperlipidemia, and atherosclerosis.Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR both in vitro and in vivo.{9823} The cis stereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50 value of 15 µM. {17615, 17566} By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.{9823}  

 

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SKU: 10011296 - 1 mg Category:

Description

A competitive antagonist of FXR (IC50 = 15 µM ) that inhibits chenodeoxycholic acid (CDCA)-induced transactivation of FXR; lowers LDL cholesterol and triglyceride levels in rodents fed a high cholesterol diet

Formal name: pregna-4-17(20)-diene-3,16-dione

Synonyms: 

Molecular weight: 312.5

CAS: 39025-24-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

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