ADX 47273

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ADX-47273 是一种对代谢型谷氨酸受体亚型 mGluR5 (EC50=170 nM) 具有选择性的正变构调节剂。

ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).

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.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 EC50 of 0.23 μM.ADX47273 (0.01-10 μM; 60 min) inhibits [3H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a Ki of 4.3 μM.

ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex.ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats.ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice.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.ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice. Animal Model:Male Long-Evans rats Dosage:1, 10 mg/kg Administration:A single i.p.Result:Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.

ADX-47273 | ADX 47273 | ADX47273

Neuroscience

GluR

mGluR5

Neurological Disease

——

851881-60-2

369.36

C20H17F2N3O2

>98% (HPLC)

Ethanol: 30 mg/mL (81.22 mM); DMSO: 74 mg/mL (200.34 mM)

O=C(C1=CC=C(F)C=C1)N2C[C@@H](C3=NC(C4=CC=C(F)C=C4)=NO3)CCC2

(S)-(4-fluorophenyl)(3-(3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)methanone

(-20℃)

With Ice Pack

≥ 2 years