VU 0361737

VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.

VU 0361737 Chemical Structure

VU 0361737 Chemical Structure

CAS: 1161205-04-4

Purity & Quality Control

Batch: S289201 DMSO] 53 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 100%
100

VU 0361737 Related Products

Signaling Pathway

Choose Selective GluR Inhibitors

Biological Activity

Description VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.
Targets
mGluR4 (Rat ) [1] mGluR4 (Human) [1]
110 nM(EC50) 240 nM(EC50)
In vitro
In vitro VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [1]
In Vivo
In vivo VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [1]
Animal Research Animal Models Sprague-Dawley rats
Dosages 10 mg/kg
Administration ip

Chemical Information & Solubility

Molecular Weight 262.69 Formula

C13H11ClN2O2

CAS No. 1161205-04-4 SDF Download VU 0361737 SDF
Smiles COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (201.75 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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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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