中文名:缬苯那嗪甲苯磺酸盐
英文名:Valbenazine tosylate
纯度:≥98%
货号:V414414
Cas号:1639208-54-0
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
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<10 μM).
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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关键字: 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)
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