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Formula | C38H54N2O10S2 |
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Molecular Weight | 762.97 | CAS No. | 1639208-54-0 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (131.06 mM) | |
Water | 25 mg/mL (32.76 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Valbenazine tosylate (NBI-98854) is the tosylate salt of valbenazine, a vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 150 nM while displaying no significant binding to VAMT1(Ki<10 μM). | ||
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Targets |
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In vitro | Valbenazine is a potent, selective, and specific inhibitor of VMAT2 with no inhibition of the related VMAT1 transporter and minimal off-target interactions at more than 80 other receptor transporters and ion channels[2]. | ||
In vivo | Valbenazine is a novel and highly selective VMAT2 inhibitor that is rapidly absorbed but more slowly metabolized, with a half-life of approximately 20 h that supports once-daily dosing[2]. Valbenazine has moderate absorption with an absolute oral bioavailability of approximately 49%; time to maximum concentration ranges from 0.5 to 1.0 hour. Valbenazine can be taken with or without food. Valbenazine exhibits protein binding of 99%. Valbenazine is primarily metabolized via the hydrolysis of the valine ester and cytochrome P450 (CYP) 3A4/5 into R,R,R-HTBZ and a mono-oxy metabolite[3]. |
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Shared GABA transmission pathology in dopamine agonist- and antagonist-induced dyskinesia [ Cell Rep Med, 2023, 4(10):101208] | PubMed: 37774703 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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