VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM.

Product information

CAS Number: 890764-63-3

Molecular Weight: 402.38

Formula: C22H15FN4O3

Chemical Name: N-[1-(2-fluorophenyl)-3-phenyl-1H-pyrazol-5-yl]-4-nitrobenzamide

Smiles: [O-][N+](=O)C1C=CC(=CC=1)C(=O)NC1=CC(=NN1C1=CC=CC=C1F)C1C=CC=CC=1

InChiKey: BRAZLURTFMCAHU-UHFFFAOYSA-N

InChi: InChI=1S/C22H15FN4O3/c23-18-8-4-5-9-20(18)26-21(14-19(25-26)15-6-2-1-3-7-15)24-22(28)16-10-12-17(13-11-16)27(29)30/h1-14H,(H,24,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

VU-1545 (10 and 100 μM) promotes AKT activation. VU-1545 at the concentrations of 0.1 and 1.0 μM efficiently promots Akt activation above basal levels.

References:

1. Tomas de Paulis, et al. Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J Med Chem. 2006 Jun 1;49(11):3332-44.
2. J G Doria, et al. Metabotropic glutamate receptor 5 positive allosteric modulators are neuroprotective in a mouse model of Huntington's disease. Br J Pharmacol. 2013 Jun;169(4):909-21.

Products are for research use only. Not for human use.