Drug intelligence / Profile preview

GW0742

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intraperitoneal (preclinical/animal Studies Only)
01

Overview

GW0742 is a **synthetic, potent, and selective agonist** of peroxisome proliferator-activated receptor beta/delta (PPARβ/δ), a member of the nuclear hormone receptor family. It acts primarily as a **PPARβ/δ agonist** but can function as a mixed agonist/antagonist at other nuclear receptors depending on dosage. GW0742 is antagonistic at the androgen receptor and vitamin D receptor (VDR), and in silico studies suggest effects on thyroid hormone receptors. Developed by GlaxoSmithKline, GW0742 has been used almost exclusively as a pharmacological tool compound in preclinical studies, with no current approved therapeutic uses. Research has demonstrated **antidiabetic, anti-inflammatory, and antihypertensive effects** in animal models, including improved insulin resistance, mitigation of liver damage, reduced neuroinflammation, protection of cardiac and vascular function, and support for metabolic homeostasis[1][3][4][6][7][8][10].

Other names
fitorine
02

Targets

AR (Adrenergic receptors)THR (Thyroid hormone receptor)PPARD (Peroxisome proliferator–activated receptor delta)PPARA (Peroxisome proliferator-activated receptor alpha)VDR (Vitamin D receptor)PPARG (Peroxisome proliferator-activated receptor gamma)

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