| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Valbenazine (formerly NBI98854; MT5199; NBI-98854; MT-5199; trade name: Ingrezza) is a potent and selective inhibitor of VMAT2 (vesicular monoamine transporter 2) with potential usefulness in the treatment of TD/tardive dyskinesia (uncontrollable movement of the face, tongue, or other body parts). As of 2017, it has been approved by FDA as the first medication to treat adults with TD/tardive dyskinesia. Valbenazine 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. Valbenazine is used to treat tardive dyskinesia in adults. Tardive dyskinesia is a neurological disorder characterized by involuntary movements. The clinical trials that led to FDA approval of valbenzazine were 6 weeks in duration. An industry-sponsored study has studied the use of valbenzazine for up to 48 weeks, in which it was found to be safe and effective for maintaining short-term (6 week) improvements in tardive dyskinesia.
| ln Vitro |
In rat striatum and human platelets, valbenazine demonstrates VMAT2 binding affinities with Kis values of 110 and 150 nM, respectively [1].
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| ln Vivo |
Oral valbenazine (10 mg/kg) causes ptosis in rats, which is mainly an adrenergic response, and raises plasma prolactin, which is primarily a dopaminergic response [1].
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| Animal Protocol |
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| References |
[1]. Dimitri E Grigoriadis, et al. Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites. J Pharmacol Exp Ther. 2017 Jun;361(3):454-461.
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| Molecular Formula |
C24H38N2O4
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| Molecular Weight |
418.57
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| CAS # |
1025504-45-3
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| Related CAS # |
Valbenazine tosylate;1639208-54-0
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| SMILES |
N[C@@H](C(C)C)C(O[C@H]1[C@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@@]2([H])C1)=O
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| Synonyms |
Valbenazine; NBI-98854; MT-5199; NBI 98854; MT5199; NBI98854; MT 5199; trade name: Ingrezza
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3891 mL | 11.9454 mL | 23.8909 mL | |
| 5 mM | 0.4778 mL | 2.3891 mL | 4.7782 mL | |
| 10 mM | 0.2389 mL | 1.1945 mL | 2.3891 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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