ADX-47273

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ADX-47273 is available in the following compound libraries:

Chemical Library (96-well) GPCR Small Molecule Compound Library (96-well) Inhibitor Library (96-well)

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Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S2251	(-)-Huperzine A	<1 mg/mL	0.66 mg/mL	<1 mg/mL
S2857	Dizocilpine (MK 801)	<1 mg/mL	67 mg/mL	7 mg/mL
S6001	LY2140023 (LY404039)	<1 mg/mL	1 mg/mL	<1 mg/mL
S1245	Dimebon (Latrepirdine)	79 mg/mL	24 mg/mL	13 mg/mL
S2690	ADX-47273	<1 mg/mL	74 mg/mL	30 mg/mL
S2795	VU 0357121	<1 mg/mL	61 mg/mL	21 mg/mL
S2809	MPEP	<1 mg/mL	39 mg/mL	39 mg/mL
S2861	CTEP	<1 mg/mL	78 mg/mL	10 mg/mL
S2876	(-)-MK 801 Maleate	<1 mg/mL	68 mg/mL	<1 mg/mL
S2862	VU 0364770	<1 mg/mL	47 mg/mL	47 mg/mL
S2892	VU 0361737	<1 mg/mL	53 mg/mL	<1 mg/mL
S7072	NMDA (N-Methyl-D-aspartic acid)	30 mg/mL	5 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	ADX47273 is a potent and specific mGlu5 antagonist with IC50 of 0.17μM.
Targets	mGlu5
IC50	0.17 μM ^[1]
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. ^[1] 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. ^[2]
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. ^[1] 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. ^[3]
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Protocol(Only for Reference)

1

References

Chemical Information

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Molecular Weight (MW)	369.36
Formula	C₂₀H₁₇F₂N₃O₂
CAS No.	851881-60-2
Synonyms	N/A

Solubility (25°C) DMSO 74 mg/mL Water <1 mg/mL Ethanol 30 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

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

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Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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Related GluR Chemicals

(-)-Huperzine A
(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with K_i of 7 nM.
VU 0357121
VU0357121 is a novel allosteric modulator of mGlu5 with EC50 of 33 nM.
MPEP
MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM.
Dizocilpine (MK 801)
Dizocilpine is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with K_i of 30.5 nM.
CTEP
CTEP is a selective allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM.
VU 0364770
VU 0364770 is a selective positive allosteric mGlu4 with EC50 of 1.1 μM.
(-)-MK 801 Maleate
MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes.
VU 0361737
VU 0361737 is a selective positive allosteric modulator for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively.
LY2140023 (LY404039)

LY404039 is a potent agonist of recombinant human mGlu2, mGlu3 receptors and rat neurons expressing native mGlu2/3 receptors with K_i of 149 nM, 92 nM and 88 nM, respectively.
NMDA (N-Methyl-D-aspartic acid)
NMDA（N-Methyl-D-aspartic acid）is a specific agonist for NMDA receptor mimicking the action of L-glutamate receptor.

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Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

ADX-47273 is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Protocol(Only for Reference)

References

Chemical Information

Research Area

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Related GluR Chemicals

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S2251	(-)-Huperzine A	<1 mg/mL	0.66 mg/mL	<1 mg/mL
S2857	Dizocilpine (MK 801)	<1 mg/mL	67 mg/mL	7 mg/mL
S6001	LY2140023 (LY404039)	<1 mg/mL	1 mg/mL	<1 mg/mL
S1245	Dimebon (Latrepirdine)	79 mg/mL	24 mg/mL	13 mg/mL
S2690	ADX-47273	<1 mg/mL	74 mg/mL	30 mg/mL
S2795	VU 0357121	<1 mg/mL	61 mg/mL	21 mg/mL
S2809	MPEP	<1 mg/mL	39 mg/mL	39 mg/mL
S2861	CTEP	<1 mg/mL	78 mg/mL	10 mg/mL
S2876	(-)-MK 801 Maleate	<1 mg/mL	68 mg/mL	<1 mg/mL
S2862	VU 0364770	<1 mg/mL	47 mg/mL	47 mg/mL
S2892	VU 0361737	<1 mg/mL	53 mg/mL	<1 mg/mL
S7072	NMDA (N-Methyl-D-aspartic acid)	30 mg/mL	5 mg/mL	<1 mg/mL

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Product Categories

ADX-47273

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

ADX-47273 is available in the following compound libraries:

Product Information

Compare GluR Chemicals

Product Description

Biological Activity

Protocol(Only for Reference)

References

Chemical Information

Research Area

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related GluR Chemicals

Neuronal Signaling Pathway Products

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