SLU-PP-915 (C007B-419161)

SLU-PP-915 is an agonist of ERR . SLU-PP-915 has an EC 50 value of approximately 400 nM for ERRα , ERRβ , and ERRγ . SLU-PP-915 has potential application in maintaining oxidative metabolism and heart failure.Form:SolidIn Vitro:SLU-PP-915 (2.5 µM; 72 h) increases the gene and protein expression of transcription factor EB (TFEB) in neonatal rat ventricular myocytes (NRVMs). SLU-PP-915 (5 µM) increases the expression of TFEB gene (at 3 h) and TFEB protein (at 72 h) in C 2 C 12 cells. SLU-PP-915 (5 µM; 48 h or 72 h) increases the expression of PGC1a, p62, PDK4, CTSD, LAMP1, LAMP2 and MCOLN1 ERR target genes in C 2 C 12 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Neonatal rat ventricular myocytes (NRVMs) and C 2 C 12 cells. Concentration: 2.5 µM and 5 µM. Incubation Time: 72 h. Result: Increased the expression of TFEB and LAMP1. ImmunofluorescenceCell Line: C 2 C 12 cells. Concentration: 5 µM. Incubation Time: 48 h. Result: Increased the expression of TFEB.In Vivo:SLU-PP-915 improves transaortic constriction (TAC) induced heart failure in adult male mice [1] . SLU-PP-915 significantly normalizes the metabolic profile of fatty acids/lipids and TCA/OXPHOS metabolites in the heart of mice with 6-week pressure overload. SLU-PP-915 improves the blood pumping function in vivo in TAC induced heart failure without affecting cardiac hypertrophy [2] . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Males C57BI/6J mice (8 weeks of age) [2] . Dosage: 20 mg/kg. Administration: Intraperitoneal injection; single dose. Result: Pharmacokinetic (PK) parameters of SLU-PP-915 in mice T max (h) C max (ng/mL) AUC last (h•ng/mL) V z /F (L/kg) CL/F (mL/min/kg) T 1/2 (h) 0.5 2813 1846 11 179 0.71. Specification: 0.98 Molecular Formula: C17H13BFNO3S Molecular Weight: 341.16