[CAS NO. 1639208-54-0]  Valbenazine tosylate

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PRODUCTS SPECIFICATIONS [1639208-54-0]

Catalog
SLK-S9500
Brand
Selleck
CAS
1639208-54-0

DESCRIPTION [1639208-54-0]

Overview

MDL-
Molecular Weight762.97
Molecular FormulaC38H54N2O10S2
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 mg5 mg10 mg
1 mM1.3107 mL6.5533 mL13.1067 mL
5 mM0.2621 mL1.3107 mL2.6213 mL
10 mM0.1311 mL0.6553 mL1.3107 mL
50 mM0.0262 mL0.1311 mL0.2621 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).

Targets

VMAT2 [1]
150 nM(Ki)

In vitro

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.