NBI-98782

NBI-98782 is a potent vesicular monoamine transporter (VMAT2) inhibitor. NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM. IC50 value: 0.97± 0.48 nM Target: VMAT2 The (+)-isomer showed high affinity in vitro (Ki = 0.97 +/- 0.48 nM) for the vesicular monoamine transporter (VMAT2) in rat brain striatum, whereas the (-)-isomer was inactive (Ki = 2.2 +/- 0.3 microM). Each isomer was then synthesized in carbon-11 labeled form, and regional brain biodistributions in mice determined after intravenous injection.

Product information

CAS Number: 85081-18-1

Molecular Weight: 319.44

Formula: C19H29NO3

Synonym:

(+)-DTBZ

(+)-α-Dihydrotetrabenazine

(+)-α-DHTBZ

NBI98782

NBI 98782

Chemical Name: (2R,3R,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-ol

Smiles: CC(C)C[C@@H]1CN2CCC3=CC(OC)=C(C=C3[C@H]2C[C@H]1O)OC

InChiKey: WEQLWGNDNRARGE-DJIMGWMZSA-N

InChi: InChI=1S/C19H29NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16-17,21H,5-7,10-11H2,1-4H3/t14-,16-,17-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Luo R, Bozigian H, Jimenez R, Loewen G, O'Brien CF. Single Dose and Repeat Once-Daily Dose Safety, Tolerability and Pharmacokinetics of Valbenazine in Healthy Male Subjects. Psychopharmacol Bull. 2017 Aug 1;47(3):44-52. PMID: 28839339; PMCID: PMC5546550.
2. Huang M, He W, Rajagopal L, Kudwa A, Grigoriadis DE, Meltzer HY. 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. Pharmacol Biochem Behav. 2020 Mar;190:172872. doi: 10.1016/j.pbb.2020.172872. Epub 2020 Feb 18. PMID: 32084491.

Products are for research use only. Not for human use.