[CAS NO. 851881-60-2] ADX-47273

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PRODUCTS SPECIFICATIONS [851881-60-2]

Catalog

SLK-S2690

Brand

Selleck

CAS

851881-60-2

DESCRIPTION [851881-60-2]

Overview

MDL	MFCD17167026
Molecular Weight	369.36
Molecular Formula	C20H17F2N3O2
SMILES	C(=O)(N1C[C@@H](C2=NC(=NO2)C3=CC=C(F)C=C3)CCC1)C4=CC=C(F)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.7074 mL	13.5369 mL	27.0739 mL
5 mM	0.5415 mL	2.7074 mL	5.4148 mL
10 mM	0.2707 mL	1.3537 mL	2.7074 mL
50 mM	0.0541 mL	0.2707 mL	0.5415 mL

Description

ADX47273 (BA 94673139) is a potent and specific positive allosteric modulator(PAM) with of 0.17 μM, showing no activity at other mGlu subtypes.

Targets

mGlu5 ^[1]

0.17 μM(EC50)

In vitro

ADX47273 causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5, the maximal increase in the response is approximately 9-fold, with an EC50 of 0.17 ± 0.03 μM. ADX47273 causes a concentration-dependent increase in the response to 300 nM glutamate with an EC50 value of 0.23 ± 0.07 μM in primary astrocyte cultures. ADX47273 at concentration of 0.1 or 1 μM decreases the EC50 for glutamate for 4- and 9-fold, respectively, in HEK 293 cells expressing rat mGlu5. ADX47273 at concentration of 1 or 3 μM decreases the EC50 for glutamate for 4- and 9-fold, respectively, in primary astrocyte cultures. ADX47273 inhibits binding of [3H]MPEP to membranes prepared from HEK 293 cells expressing mGlu5 receptors with Ki of 4.3 ± 0.5 μM. ADX-47273 at concentration of 0.3 μM elicited an enhancement of NMDA-receptor dependent long-term potentiation in rat hippocampal slices, the effect can be blocked in the presence of 10 μM specific mGlu5 receptor antagonist MPEP.

In vivo

ADX47273 intraperitoneally administrated at dose of 10 mg/kg increases ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus in Long-Evans rats. ADX47273 intraperitoneally administrated at dose of 10-100 mg/kg produces dose-dependent decreases in avoidance responding and increased escapes at doses that did not produce any response failures in Sprague-Dawley rats. ADX47273 intraperitoneally administrated at dose of 10-300 mg/kg produces a dose-dependent decrease in apomorphine-induced climbing in CF-1 mice. ADX47273 intraperitoneally administrated at dose of 100 mg/kg decreased locomotor activity compared with vehicle pretreatment at 20 min after PCP, 30 min after apomorphine, and at all time points after amphetamine challenge in mice. ADX47273 intraperitoneally administrated at dose of 175 mg/kg lowers dopamine levels in the Sprague-Dawley rat nucleus accumbens. ADX47273 intraperitoneally administrated at dose of 1 to 50 mg/kg increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats. ADX47273 intraperitoneally administrated at dose of 100 mg/kg signiﬁcantly decreases conditioned avoidance response at 30 and 90 min post-injection in male Sprague-Dawley rats.

References

[1] Liu F, et al. J Pharmacol Exp Ther, 2008, 327(3), 827-839.
[2] Rosenbrock H, et al. Eur J Pharmacol, 2010, 639(1-3), 40-6.
[3] Schlumberger C, et al. Pharmacol Biochem Behav, 2010, 95(1), 23-30.

Synonyms

Methanone, (4-fluorophenyl)[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]-

Piperidine, 1-(4-fluorobenzoyl)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-, (3S)-

(4-Fluorophenyl)[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]methanone

ADX 47273

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