Bioactivity | 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 hypertension[1]. |
Target | IC50: 92 nM Specific E3ubiquitin protein ligase 1 (SMURF1) |
In Vivo | Smurf1-IN-1 (Compound 38) (1,3,10 mg/kg,口服) 对大鼠肺部高压模型有显著疗效[1]。Smurf1-IN-1 (静脉注射1 mg/kg,口服 3 mg/kg) 显示 T1/2 为 7.9 小时,口服生物利用度 (F%) 为 82%[1]。 Animal Model: |
Name | Smurf1-IN-1 |
CAS | 1824708-03-3 |
Formula | C24H29ClN6O2 |
Molar Mass | 468.98 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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 Hypertension. J Med Chem. 2023 Jun 22;66(12):8130-8139. |