[CAS NO. 2597958-02-4] Glucosylceramidesynthase-IN-2
PRODUCTS SPECIFICATIONS [2597958-02-4]
DESCRIPTION [2597958-02-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 447.41 |
| Molecular Formula | C22H20F3N3O4 |
| SMILES | O=C(C1=CC=NN(C1=O)C2=C(OCC(F)(F)F)C=CC=C2)NC3=CC=C(C(C)(O)C)C=C3 |
Summary
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 [1] .
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)
[1]
.
Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, Ca
V
1.2, and Na
V
1.5 channels
[1]
.
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
[1]
.
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%)
[1]
.
Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 μM at 30 mg/kg dosing, 1 h)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)