A ligand of RXR that acts as an antagonist towards RXR homodimers but as an agonist of heterodimers consisting of RXR and RAR or PPARs; strongly enhances signaling through RXR-PPARγ in response to PPARγ ligands

LG 100754 – 25 mg

Brand:
Cayman
CAS:
180713-37-5
Storage:
-20
UN-No:
Non-Hazardous - /

LG 100754 is a ligand of retinoid X receptor (RXR) that modulates the activity of RXR dimers. It acts as an antagonist towards RXR homodimers but as an agonist of heterodimers consisting of RXR and retinoic acid receptor (RAR) or PPARs.{33119,33120,33121} LG 100754, at 1 µM, is a weak agonist of RXR-PPARγ but strongly enhances signaling through the heterodimer in response to PPARγ ligands, including rosiglitazone (Item No. 71740) and 15-deoxy-Δ12,14-prostaglandin J2 (Item No. 18570).{33118} Through this action, LG 100754 decreases glucose levels and relieves insulin resistance in mice.{33117,33118}  

 

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Description

A ligand of RXR that acts as an antagonist towards RXR homodimers but as an agonist of heterodimers consisting of RXR and RAR or PPARs; strongly enhances signaling through RXR-PPARγ in response to PPARγ ligands

Formal name: 3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-2-naphthalenyl)-2E,4E,6Z-octatrienoic acid

Synonyms:  CD3159|LGD 100754|UVI2112

Molecular weight: 396.6

CAS: 180713-37-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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