1. Neuronal Signaling
  2. Glucosylceramide Synthase (GCS)
  3. Glucosylceramide synthase-IN-3

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.

For research use only. We do not sell to patients.

Glucosylceramide synthase-IN-3 Chemical Structure

Glucosylceramide synthase-IN-3 Chemical Structure

CAS No. : 3029827-91-3

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Description

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[1][2].

In Vitro

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[1].
Glucosylceramide synthase-IN-2 has the IC50 of 20 nM in primary neurons[1].
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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)[1].
Glucosylceramide synthase-IN-2 (6, 20 or 100 mg/kg/day for 4 days; oral gavage) causes larger reductions in GlcCer[1].
Glucosylceramide synthase-IN-2 has good pharmaceutical properties with high permeability (pApp=26.54) and is not a substrate of P-gp[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

381.40

Formula

C21H20FN3O3

CAS No.
SMILES

O=C(O[C@H]1CN2CCC1CC2)NC3=CC=CC4=C3N=C(O4)C5=CC=C(C=C5)F

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Glucosylceramide synthase-IN-3 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Glucosylceramide synthase-IN-3
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HY-144270
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