NBI-98782 |
Catalog No.GC36705
One-Click Copy Product Info
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NBI-98782 is a potent and selective vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 3nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 85081-18-1
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 85081-18-1 | SDF | |
| Canonical SMILES | COC(C=C1CCN2C[C@@H](CC(C)C)[C@@H]3O)=C(C=C1[C@]2(C3)[H])OC | ||
| Formula | C19H29NO3 | M.Wt | 319.44 |
| Solubility | DMSO: 33.33 mg/mL (104.34 mM) | Storage | Store at -20°C; protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1305 mL | 15.6524 mL | 31.3048 mL |
| 5 mM | 626.1 μL | 3.1305 mL | 6.261 mL |
| 10 mM | 313 μL | 1.5652 mL | 3.1305 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)