Glucosylceramide synthase-IN-2

Names

[ Name ]:
Glucosylceramide synthase-IN-2

Biological Activity

[Description]:

Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s 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[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

[In Vitro]

Glucosylceramide synthase-IN-2 (compound T-690) has no SERT inhibitory activity (IC50>10 μM). Glucosylceramide synthase-IN-2 does not affect GCase activity (EC50>300 μM)[1]. Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, CaV1.2, and NaV1.5 channels[1].

[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[1]. Glucosylceramide synthase-IN-2 (po; 5 mg/kg) has a Cmax of 416 ng/mL. Glucosylceramide synthase-IN-2 shows good oral exposure (BA = 31%)[1]. Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 μM at 30 mg/kg dosing, 1 h)[1].

[References]

[1]. Yuta Tanaka, et al. Discovery of Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore. J Med Chem. 2022 Mar 10;65(5):4270-4290

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₀F₃N₃O₄

[ Molecular Weight ]:
447.41

Related Compounds

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