VU0469650

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0469650 

VU0469650 是一种有效的、选择性的、穿透 CNS 的 mGlu1 受体的反向变构调节剂,其 IC50 为99 nM。

VU0469650

VU0469650 Chemical Structure

CAS No. : 1443748-47-7

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生物活性

VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM[1].

IC50 & Target

mGluR 1

99 nM (IC50)

体内研究
(In Vivo)

VU0469650 (male Sprague-Dawley rats, 0.2 mg/kg, IV, once) exhibits moderate to high clearance, a moderate volume of distribution, and a half-life of approximately 1 hour[1].
VU0469650 (male Sprague-Dawley rats, 10 mg/kg, IP, once) shows an excellent selectivity profile and good exposure in both plasma and brain samples[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

364.48

Formula

C22H28N4O

CAS 号

1443748-47-7

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.

参考文献
  • [1]. Lovell KM, Felts AS, Rodriguez AL, et al. N-Acyl-N’-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718.

Animal Administration

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Lovell KM, Felts AS, Rodriguez AL, et al. N-Acyl-N’-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718.

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