Description
STL1267 is a potent and cross-the-blood-brain barrier REV-ERB agonist with a K i value of 0.16 µM for REV-ERBα. STL1267 shows no cytotoxicity. STL1267 inhibits the gene expression of BMAL1In VitroSTL1267 (5 µM; 24 h) decreases the expression of BMAL1 and increases the gene expression of Mtnd1, Mtco1, Vicad, Lcad, Scad, Lkb1, Sirt1, Nampt, Ppargc1a in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HepG2, C2C12 cells Concentration: 0-20 µM Incubation Time: 24 h Result: Showed no adverse effects on cell viability up to the maximum dose examined 20 µM. RT-PCRCell Line: HepG2 cells Concentration: 5 µM Incubation Time: 24 h Result: Decreased the gene expression of BMAL1, increased the gene expression of Mtnd1, Mtco1, Vicad, Lcad, Scad, Lkb1, Sirt1, Nampt, Ppargc1a.In VivoSTL1267 (50 mg/kg; i.p.; once) inhibits Bmal1 expression in mouse. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks, male C57Bl/6 J mice Dosage: 50 mg/kg Administration: I.p.; once Result: Showed a plasma half-life of 1.6 h, effectively suppressed BMAL1 expression in the liver at 12 h post-administration.Form:SolidIC50& Target:K i : 0.16 µM (REV-ERBα)