VU0364289

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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。

CAS NO:

1242443-29-3

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].

	T_max(h)	C_max(ng/mL)	Plasma protein binding	Rat Fu (free fraction)
IP (10 mg/kg)	0.25	1280	94% (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.