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Catalog:
SLK-S9500
Brand:
Selleck
CAS:
1639208-54-0
Overview
MDL
-
Molecular Weight
762.97
Molecular Formula
C38H54N2O10S2
SMILES
-
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
1.3107 mL
6.5533 mL
13.1067 mL
5 mM
0.2621 mL
1.3107 mL
2.6213 mL
10 mM
0.1311 mL
0.6553 mL
1.3107 mL
50 mM
0.0262 mL
0.1311 mL
0.2621 mL
Description
Valbenazine tosylate (NBI-98854) is the tosylate salt of valbenazine, a inhibitor with a Ki value of 150 nM while displaying no significant binding to VAMT1(Ki<10 μM).
Valbenazine is a potent, selective, and specific inhibitor of VMAT2 with no inhibition of the related VMAT1 transporter and minimal off-target interactions at more than 80 other receptor transporters and ion channels.
In vivo
Valbenazine is a novel and highly selective VMAT2 inhibitor that is rapidly absorbed but more slowly metabolized, with a half-life of approximately 20 h that supports once-daily dosing. Valbenazine has moderate absorption with an absolute oral bioavailability of approximately 49%; time to maximum concentration ranges from 0.5 to 1.0 hour. Valbenazine can be taken with or without food. Valbenazine exhibits protein binding of 99%. Valbenazine is primarily metabolized via the hydrolysis of the valine ester and cytochrome P450 (CYP) 3A4/5 into R,R,R-HTBZ and a mono-oxy metabolite.
