Glucosylceramide synthase-IN-2

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 Vitro Glucosylceramide 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 Vivo Glucosylceramide 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

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