GLPBio

NBI-98782

Catalog No.: GC36705Purity:>98.50%
COASDSData Sheet
NBI-98782 is a potent and selective vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 3nM.

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NBI-98782
Cas No.: 85081-18-1
10mM (in 1mL DMSO)In Stock
$60.00
1
1mgIn Stock
$28.00
1
5mgIn Stock
$55.00
1
10mgIn Stock
$88.00
1
25mgIn Stock
$160.00
1
50mgIn Stock
$220.00
1
100mgIn Stock
$297.00
1
200mgIn Stock
$401.00
1
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Description

NBI-98782 is a potent and selective vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 3nM [1]. NBI-98782 reduces the packaging of monoamines by targeting VMAT2, thereby leading to a decrease in monoamine release and neural transmission[2]. NBI-98782 has been widely used to promote ptosis in rats, stimulate prolactin secretion, and regulate neural functions[3].

In vivo, NBI-98782 treatment via oral administration at a dose of 10mg/kg/day for 7 days significantly decreased basal levels of dopamine and serotonin, and enhanced the release of acetylcholine and GABA levels in mice [4].

References:
[1] Meyer J M. Valbenazine for tardive dyskinesia[J]. Curr Psychiatr, 2017, 16(5): 40-46.
[2] Terry-Lorenzo R, Albrecht D, Crouch S, et al. Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study[J]. Neuropsychopharmacology, 2025, 50(7): 1093-1101.
[3] Grigoriadis D E, Smith E, Hoare S R J, et al. Pharmacologic characterization of valbenazine (NBI-98854) and its metabolites[J]. The Journal of Pharmacology and Experimental Therapeutics, 2017, 361(3): 454-461.
[4] Huang M, He W, Rajagopal L, et al. Effects of NBI-98782, a selective vesicular monoamine transporter 2 (VMAT2) inhibitor, on neurotransmitter efflux and phencyclidine-induced locomotor activity: Relevance to tardive dyskinesia and antipsychotic action[J]. Pharmacology Biochemistry and Behavior, 2020, 190: 172872.

Protocol

Animal experiment [1]:

Animal models

Male C57BL/6 J mice

Preparation Method

Male C57BL/6 J mice, weighing 20-25g, were group housed (four per cage) in a controlled environment held at 21±2°C and 50±15% relative humidity on a 14/10h light-dark cycle. Food and water were available ad libitum. NBI-98782 and tetrabenazine were dissolved in 30% propylene glycol and 20% polyethylene glycol 400 in 0.25% methyl cellulose (400cps) in water. NBI-98782 was orally administered (10mg/kg/day) for 7 days. Microdialysis was performed on the 8th day.

Dosage form

10mg/kg/day for 7 days; p.o.

Applications

NBI-98782 treatment significantly decreased basal levels of dopamine and serotonin, with a trend to decrease norepinephrine levels in mice.

References:
[1] Huang M, He W, Rajagopal L, et al. Effects of NBI-98782, a selective vesicular monoamine transporter 2 (VMAT2) inhibitor, on neurotransmitter efflux and phencyclidine-induced locomotor activity: Relevance to tardive dyskinesia and antipsychotic action[J]. Pharmacology Biochemistry and Behavior, 2020, 190: 172872.

Product Documents

Purity:>98.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
85081-18-1
SMILES
COC(C=C1CCN2C[C@@H](CC(C)C)[C@@H]3O)=C(C=C1[C@]2(C3)[H])OC
Molecular Formula
C19H29NO3
Molecular Weight
319.44
Solubility
DMSO: 33.33 mg/mL (104.34 mM)
Storage
Store at -20°C; protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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