Home Neuronal Signaling GluR agonist VU 0357121

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VU 0357121 GluR agonist

Cat.No.S2795

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.
VU 0357121 GluR agonist Chemical Structure

Chemical Structure

Molecular Weight: 305.32

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Quality Control

Batch: S279501 DMSO]61 mg/mL]false]Ethanol]21 mg/mL]false]Water]Insoluble]false Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 21 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 305.32 Formula

C17H17F2NO2

 Storage (From the date of receipt)
CAS No. 433967-28-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCCCOC1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)F)F

Mechanism of Action

Targets/IC50/Ki
mGluR5
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. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line.
References

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