Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary pertension.
Smurf1-IN-1 (Compound 38) (1, 3, 10 mg/kg for p.o.) has significant efficacy in rats model of pulmonary pertension[1].Smurf1-IN-1 (1 mg/kg for i.v., 3 mg/kg for p.o.) shows a T1/2 of 7.9, and oral bioavailability of 82%[1]. Pharmacokinetic parameters for Smurf1-IN-1 (Compound 38) in rats [1]
References:
[1]. Shaw DE, et.al. Design and Synthesis of Inhibitors of the E3 Ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 as a Treatment for Lung Remodeling in Pulmonary Arterial pertension. J Med Chem. 2023 Jun 22;66(12):8130-8139.