2597958-02-4
2597958-02-4 structure
- Name: Glucosylceramide synthase-IN-2
- Chemical Name: Glucosylceramide synthase-IN-2
- CAS Number: 2597958-02-4
- Molecular Formula: C22H20F3N3O4
- Molecular Weight: 447.41
- Catalog: Research Areas Metabolic Disease
- Create Date: 2022-04-24 16:06:48
- Modify Date: 2024-01-10 12:03:32
-
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].
| Name | Glucosylceramide synthase-IN-2 |
|---|
| 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 | |
| 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 |
| Molecular Formula | C22H20F3N3O4 |
|---|---|
| Molecular Weight | 447.41 |