Description
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC 50 s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research.In VitroGlucosylceramide synthase-IN-2 (compound T-690) has no SERT inhibitory activity (IC 50 >10 µM). Glucosylceramide synthase-IN-2 does not affect GCase activity (EC 50 >300 µM). Glucosylceramide synthase-IN-2 (30 µM) does not potently inhibit hERG, Ca V 1.2, and Na V 1.5 channels. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGlucosylceramide synthase-IN-2 (compound T-690; po; 30, 100, 300 mg/kg) reduces GlcCer concentrations in the plasma and cerebral cortex in a dose-dependent manner in C57BL/6J mice. Glucosylceramide synthase-IN-2 (po; 5 mg/kg) has a C max of 416 ng/mL. Glucosylceramide synthase-IN-2 shows good oral exposure (BA = 31%). Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 µM at 30 mg/kg dosing, 1 h). MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:Solid