您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > VU0364289
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
VU0364289
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VU0364289图片
CAS NO:1242443-29-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
VU0364289 是一种与 MPEP (HY-14609A) 位点结合的高选择性mGlu5正性变构调节剂,其EC50值为 1.6 μM。VU0364289 能以剂量依赖的方式逆转小鼠模型中 Amphetamine 诱导的过度运动,可用于精神分裂症和其他精神病学研究。
生物活性

VU0364289 is a highly selectivemGlu5positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with anEC50of 1.6 μM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research[1][2][3].

IC50& Target

mGlu5

1.6 μM (EC50)

体内研究
(In Vivo)

VU0364289 (10, 30, 56.6, 100 mg/kg ; i.p.; once) reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, and (56.6, 100 mg/kg) shows significantly fewer ambulations[1].
VU0364289 (10 mg/kg; i.p.; once) is rapidly and significantly absorbed in rats, and shows excellent central nervous system penetration[1].

Animal Model:Adult male Sprague-Dawley rats (250-275 g)[1].
Dosage:10, 30, 56.6, 100 mg/kg
Administration:Intraperitoneal injection; once.
Result:Showed activity of reversing the hyperlocomotion induced by amphetamine, and can also significantly fewer ambulations in rats when dose up to 56.6 mg/kg.
Animal Model:Adult male Sprague-Dawley rats (250-275 g)[1].
Dosage:10 mg/kg
Administration:Intraperitoneal injection; once.
Result:1.19Pharmacokinetic Parameters of VU0364289 in male Sprague-Dawley rats[1].
Tmax(h)Cmax(ng/mL)Plasma protein bindingRat Fu (free fraction)
IP (10 mg/kg)0.25128094% (h); 90% (r)0.10
分子量

335.40

Formula

C20H21N3O2

CAS 号

1242443-29-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.