aladdin 阿拉丁 V414414 缬苯那嗪甲苯磺酸盐 1639208-54-0 98%

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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