Glucosylceramide-IN-2 (T-690) is a potent, blood-brain barrier-transparent and orally active inhibitor of glucosylceramide synthase (GCS) with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively. basal and non-competitive with UDP-glucose.
| Molecular Weight | 447.41 |
| Formula | C22H20F3N3O4 |
| CAS Number | 2597958-02-4 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] Maria C Messner, et al. Adv Exp Med Biol. Glucosylceramide in humans
| Related Glucosylceramide Synthase Products |
|---|
| G43
G43 is a potent, selective glucosyltransferase inhibitor, with the Kd of 3.7μM and 46.9 nM for GtfB and GtfC, respectively. |
| Glucosylceramide synthase-IN-1
Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research. |
| D-threo-PDMP
D-threo-PDMP is a potent glucoceramide synthase (GCS) inhibitor, which reduces the glycosphingolipids on the cell surface by inhibiting glycosylation, reduces the total length of the axon plexus and the number of axon branch points, and inhibits neurite growth. |
| Lucerastat
Lucerasta is the galactose form of Miglustat, an orally active inhibitor of glucosylceramide synthase (GCS).Lucerastat has potential for use in Fabry disease research. |
| Ibiglustat (L-Malic acid)
Ibiglustat (Venglustat) L-Malic acid is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. |
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