An orally bioavailable inhibitor of sEH (IC50 = 0.33 µM) and agonist of PPARγ (EC50 of 0.3 µM); water soluble

RB394 – 1 mg

Brand:
Cayman
CAS:
1830320-32-5
Storage:
-20
UN-No:
Non-Hazardous - /

RB394 is an orally bioavailable, dual modulator of soluble epoxide hydrolase (sEH) and PPARγ that inhibits sEH with an IC50 of 0.33 µM and activates PPARγ with an EC50 of 0.3 µM.{31308} It is inactive at PPARδ and shows 29% activation of PPARα, relative to control, at 10 µM.{31308} RB394 is water soluble, orally bioavailable, and can be delivered through drinking water. In a two week in vivo pharmacokinetic study in mice, 30 mg/kg body weight in drinking water resulted in a final plasma concentration of ~3 µM.{31308} This coincided with upregulation of PPARγ target genes, as well as PPARα and PPARδ, in mouse livers.{31308}  

 

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Description

An orally bioavailable inhibitor of sEH (IC50 = 0.33 µM) and agonist of PPARγ (EC50 of 0.3 µM); water soluble, orally bioavailable, and can be delivered through drinking water to upregulate PPARγ target genes

Formal name: α-ethyl-4-[[[[4-methoxy-2-(trifluoromethyl)phenyl]methyl]amino]carbonyl]-benzenepropanoic acid

Synonyms: 

Molecular weight: 409.4

CAS: 1830320-32-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs

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