Information Valbenazine tosylate 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 Targets VMAT2 150 nM(Ki) 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. 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. 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.
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Valbenazine tosylate
CAS number：1639208-54-0 molecular formula：C38H54N2O10S2
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | L-Valine, (2R,3R,11bR)-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo(a)quinolizin-2-yl ester, 4-methylbenzenesulfonate (1:2) | Q27262815 | Valbenazine (tosylate) | Ingrezza (TN) | D10999 | VALBENAZINE TOSILATE [WHO-DD] | 1639208-54-0 | ||
| CAS number | 1639208-54-0 | molecular formula | C38H54N2O10S2 |
| molecular weight | 762.97 g/mol | Exact mass | 10mM in DMSO |
| PSA | 200.000 Ų | logp | 7.062 |
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