Drug intelligence / Profile preview

RB394

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

RB394 is an orally bioavailable small molecule that acts as a dual modulator of soluble epoxide hydrolase (sEH) and peroxisome proliferator-activated receptor gamma (PPARγ). It inhibits sEH with an IC50 of 0.33 μM and activates PPARγ with an EC50 of 0.3 μM, while showing minimal activity at PPARδ and partial activation of PPARα at higher concentrations. sEH is involved in the metabolism of endogenous lipid epoxides, particularly in adipose tissue, influencing vascular relaxation through the arachidonic acid cascade. PPARγ plays a key role in adipogenesis, lipid metabolism regulation, glucose homeostasis, and anti-inflammatory processes. In preclinical studies, RB394 has demonstrated promotion of adipocyte browning, cardioprotective effects, upregulation of metabolic target genes in mouse liver, and potential for treating diabetic complications[1][2][5][7].

02

Targets

EPHX2 (Soluble epoxide hydrolase)PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)

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