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ADX-47273
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。
ADX-47273图片
CAS NO:851881-60-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
ADX-47273 是一种有效的,选择性和可透过血脑屏障的mGluR5阳性变构调节剂 (PAM),增强谷氨酸 (50 nM) 反应的EC50值为 0.17 μM。 ADX-47273 具有抗精神病和增强认知的活性。
生物活性

ADX-47273 is a potent, selective and brain-penetrantmGluR5positive allosteric modulator (PAM), with anEC50of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities[1][2].

IC50& Target[1]

mGluR5

0.17 μM (EC50)

体外研究
(In Vitro)

ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5 without eliciting a response by itself[1].
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 300 nM glutamate in primary astrocyte cultures, with an EC50of 0.23 μM[1].
ADX47273 (0.01-10 μM; 60 min) inhibits [3H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a Kiof 4.3 μM[1].

体内研究
(In Vivo)

ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex[1].
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats[1].
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice[1].
ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats[1].
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice[3].

Animal Model:Male Long-Evans rats[1]
Dosage:1, 10 mg/kg
Administration:A single i.p.
Result:Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.
分子量

369.36

性状

Solid

Formula

C20H17F2N3O2

CAS 号

851881-60-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL(83.93 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7074 mL13.5369 mL27.0739 mL
5 mM0.5415 mL2.7074 mL5.4148 mL
10 mM0.2707 mL1.3537 mL2.7074 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。