Valbenazine - CAS 1025504-45-3
Catalog number: B0084-474971
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H38N2O4
Molecular Weight:
418.57
COA:
Inquire
Targets:
Vesicular monoamine transporter 2 (VMAT2)
Description:
Valbenazine is a potent and highly selective vesicular monoamine transporter 2(VMAT2) inhibitor. It is a prodrug of the (+)-α isomer of tetrabenazine for tardive syndrome therapy. It is effective in regulating the levels of dopamine release during nerve communication, while at the same time having minimal impact on the other monoamines. It significantly improved tardive dyskinesia and was well tolerated in patients. It is an experimental drug being investigated for use in the treatment of tardive dyskinesia and Tourette syndrome. It was developed by Neurocrine Biosciences.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474971 10 mg $199 In stock
Bulk Inquiry
Purity:
>98 %
Appearance:
Light Yellow to Yellow Solid
Synonyms:
[(2R,3R,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-yl] (2S)-2-amino-3-methylbutanoate;NBI-98854;NBI98854;MT-5199;MT5199; NBI 98854;MT 5199
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Valbenazine is an experimental drug being investigated for use in the treatment of tardive dyskinesia and Tourette syndrome.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
507.2±50.0 °C | Condition: Press: 760 Torr
Density:
1.11±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
GEJDGVNQKABXKG-CFKGEZKQSA-N
InChI:
InChI=1S/C24H38N2O4/c1-14(2)9-17-13-26-8-7-16-10-21(28-5)22(29-6)11-18(16)19(26)12-20(17)30-24(27)23(25)15(3)4/h10-11,14-15,17,19-20,23H,7-9,12-13,25H2,1-6H3/t17-,19-,20-,23+/m1/s1
Canonical SMILES:
CC(C)CC1CN2CCC3=CC(=C(C=C3C2CC1OC(=O)C(C(C)C)N)OC)OC
Current Developer:
Valbenazine was developed by Neurocrine Biosciences.
1.New findings in pharmacogenetics of schizophrenia.
Zai CC;Tiwari AK;Zai GC;Maes MS;Kennedy JL Curr Opin Psychiatry. 2018 May;31(3):200-212. doi: 10.1097/YCO.0000000000000417.
PURPOSE OF REVIEW: ;This review highlights recent advances in the investigation of genetic factors for antipsychotic response and side effects.;RECENT FINDINGS: ;Antipsychotics prescribed to treat psychotic symptoms are variable in efficacy and propensity for causing side effects. The major side effects include tardive dyskinesia, antipsychotic-induced weight gain (AIWG), and clozapine-induced agranulocytosis (CIA). Several promising associations of polymorphisms in genes including HSPG2, CNR1, and DPP6 with tardive dyskinesia have been reported. In particular, a functional genetic polymorphism in SLC18A2, which is a target of recently approved tardive dyskinesia medication valbenazine, was associated with tardive dyskinesia. Similarly, several consistent findings primarily from genes modulating energy homeostasis have also been reported (e.g. MC4R, HTR2C). CIA has been consistently associated with polymorphisms in the HLA genes (HLA-DQB1 and HLA-B). The association findings between glutamate system genes and antipsychotic response require additional replications.;SUMMARY: ;The findings to date are promising and provide us a better understanding of the development of side effects and response to antipsychotics.
2.Valbenazine as the first and only approved treatment for adults with tardive dyskinesia.
Sarva H;Henchcliffe C Expert Rev Clin Pharmacol. 2018 Mar;11(3):209-217. doi: 10.1080/17512433.2018.1429264. Epub 2018 Jan 23.
Valbenazine is a selective VMAT2 inhibitor that the FDA approved in April 2017 for the specific treatment of tardive dyskinesia (TD), a movement disorder commonly caused by dopamine blocking agents. Valbenazine acts to decrease dopamine release, reducing excessive movement found in TD. Areas covered: This drug profile reviews the development of valbenazine and the clinical trials that led to its approval as the first treatment specific to TD. The literature search was performed with the PubMed online database. Expert commentary: Two clinical trials assessing the efficacy of valbenazine have shown the reduction of antipsychotic-induced involuntary movement. No life threatening adverse effects were found. Data from a 42-week extension study demonstrated sustained response.
3.VMAT2 Inhibitors for Tardive Dyskinesia-Practice Implications.
Peckham AM;Nicewonder JA J Pharm Pract. 2018 Jan 1:897190018756512. doi: 10.1177/0897190018756512. [Epub ahead of print]
Tardive dyskinesia is a potentially irreversible, debilitating, hyperkinetic movement disorder that can result from dopamine receptor antagonists. Prompt recognition and resolution of symptoms are instrumental in preventing disease irreversibility, though current treatment options have fallen short of robust, effective, and long-term symptom control. In April 2017, the Food and Drug Administration (FDA) approved 2 new vesicular monoamine transporter 2 (VMAT2) inhibitors, deutetrabenazine and valbenazine, for chorea related to Huntington's disease and tardive dyskinesia, respectively. These agents were pharmacologically modified from tetrabenazine, a VMAT2 inhibitor used off-label in the treatment of tardive dyskinesia. Despite FDA-labeled indications of deutetrabenazine and valbenazine, each agent was explored as a treatment option for those with tardive dyskinesia. In this study, the pharmacologic modifications of the 2 new VMAT2 inhibitors are described, with detailed explanation as to how these may impact clinical practice. The associated case series, observational studies, and clinical trials exploring their use in the treatment of tardive dyskinesia are reported with expert opinion on practice implication.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Vesicular monoamine transporter 2 (VMAT2) Products


FFN 200 dihydrochloride

FFN 200 dihydrochloride is a selective fluorescent VMAT2 substrate that traces exocytosis in dopaminergic neuronal cell culture and brain tissue.

CAS 1025504-45-3 Valbenazine

Valbenazine
(CAS: 1025504-45-3)

Valbenazine is a potent and highly selective vesicular monoamine transporter 2(VMAT2) inhibitor. It is a prodrug of the (+)-α isomer of tetrabenazine for tardiv...

CAS 1004548-96-2 FFN 511

FFN 511
(CAS: 1004548-96-2)

FFN 511 is a fluorescent false neurotransmitter (FFN) targeting neuronal vesicular monoamine transporter (VMAT) 2 to inhibit serotonin binding to VMAT2 (IC50 = ...

FFN 102 mesylate

FFN 102 mesylate is a selective dopamine transporter (DAT) and VMAT2 substrate with no significant binding to a panel of 38 CNS receptors.

CAS 1883548-88-6 FFN 206 dihydrochloride

FFN 206 dihydrochloride
(CAS: 1883548-88-6)

FFN 206 dihydrochloride is a fluorescent VMAT2 substrate (IC50 app = 1.15 μM) that detects VMAT2 activity in intact cells.

Chemical Structure

CAS 1025504-45-3 Valbenazine

Quick Inquiry

Verification code

Featured Items