Home Transmembrane Transporters VMAT inhibitor Valbenazine tosylate For research use only.

Valbenazine tosylate

Synonyms: NBI-98854

Valbenazine tosylate (NBI-98854) is the tosylate salt of valbenazine, a vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 150 nM while displaying no significant binding to VAMT1(Ki<10 μM).

Valbenazine tosylate Chemical Structure

Valbenazine tosylate Chemical Structure

CAS: 1639208-54-0

Selleck's Valbenazine tosylate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 98.63%
98.63

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Biological Activity

Description Valbenazine tosylate (NBI-98854) is the tosylate salt of valbenazine, a vesicular monoamine transporter 2 (VMAT2) 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
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[2].
In Vivo
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[2]. 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[3].

Chemical lnformation & Solubility

Molecular Weight 762.97 Formula

C38H54N2O10S2
CAS No. 1639208-54-0 SDF --
Smiles CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CC(C)CC1CN2CCC3=CC(=C(C=C3C2CC1OC(=O)C(C(C)C)N)OC)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (131.06 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 25 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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