VU 0357121

Catalog No.S2795

VU 0357121 Chemical Structure

Molecular Weight(MW): 305.32

VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 110 In stock
USD 470 In stock
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Biological Activity

Description VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
Targets
mGluR5 [1]
30 nM(EC50)
In vitro

VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. [1] VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. [2]

Protocol

Solubility (25°C)

In vitro DMSO 61 mg/mL (199.79 mM)
Ethanol 21 mg/mL (68.78 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 305.32
Formula

C17H17F2NO2

CAS No. 433967-28-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

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

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GluR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID