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编 号：F762911
分子式：C21H20FN3O3
分子量：381.4
分子式：C21H20FN3O3
分子量：381.4
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CAS No: 3029827-91-3
产品详情
生物活性：
Glucosylceramide synthase-IN-3 (compound BZ1) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 16 nM for human GCS.Glucosylceramide synthase-IN-3 can be used for Gaucher's disease research.
体内研究：
Eight hours after a single dose of Glucosylceramide synthase-IN-2 (compound BZ1; 6, 20 or 100?mg/kg; oral gavage; formulated in 30%?captisol), plasma GlcCer C:16:0 is reduced in a dose-dependent fashion up to ~75% of concentration in vehicle treated animals. Brain GlcCer is also significantly reduced to concentrations of ~48% of vehicle treated controls in C57BL6 mice (8?weeks of age, male).Glucosylceramide synthase-IN-2 (6, 20 or 100?mg/kg/day for 4 days; oral gavage) causes larger reductions in GlcCer. Glucosylceramide synthase-IN-2 has good pharmaceutical properties with high permeability (pApp=26.54) and is not a substrate of P-gp.
体外研究：
Glucosylceramide synthase-IN-2 (compound BZ1) causes measuring the reduction of glucosylceramide and the cellular IC50?was determined to be 94?nM in human and 160?nM in mouse with cellular activity was confirmed using a fibroblast assay. Glucosylceramide synthase-IN-2 has the IC50?of 20?nM in primary neurons. Glucosylceramide synthase-IN-2 (10, 30, 100, 300 nM) produces a dose-dependent reduction in glycosphingolipids in WT and D409V mouse cortical neurons. Glucosylceramide synthase-IN-2 decreases the amount of detergent-insoluble pS129 α-syn.
Glucosylceramide synthase-IN-3 (compound BZ1) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 16 nM for human GCS.Glucosylceramide synthase-IN-3 can be used for Gaucher's disease research.
体内研究：
Eight hours after a single dose of Glucosylceramide synthase-IN-2 (compound BZ1; 6, 20 or 100?mg/kg; oral gavage; formulated in 30%?captisol), plasma GlcCer C:16:0 is reduced in a dose-dependent fashion up to ~75% of concentration in vehicle treated animals. Brain GlcCer is also significantly reduced to concentrations of ~48% of vehicle treated controls in C57BL6 mice (8?weeks of age, male).Glucosylceramide synthase-IN-2 (6, 20 or 100?mg/kg/day for 4 days; oral gavage) causes larger reductions in GlcCer. Glucosylceramide synthase-IN-2 has good pharmaceutical properties with high permeability (pApp=26.54) and is not a substrate of P-gp.
体外研究：
Glucosylceramide synthase-IN-2 (compound BZ1) causes measuring the reduction of glucosylceramide and the cellular IC50?was determined to be 94?nM in human and 160?nM in mouse with cellular activity was confirmed using a fibroblast assay. Glucosylceramide synthase-IN-2 has the IC50?of 20?nM in primary neurons. Glucosylceramide synthase-IN-2 (10, 30, 100, 300 nM) produces a dose-dependent reduction in glycosphingolipids in WT and D409V mouse cortical neurons. Glucosylceramide synthase-IN-2 decreases the amount of detergent-insoluble pS129 α-syn.
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