A positive allosteric modulator of mGluR5 (Ki = 195 nM); selective for mGluR5 over mGluR1

VU0360172 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1309976-62-2
Storage:
-20
UN-No:
Non-Hazardous - /

VU036172 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5; Ki = 195 nM).{47575} It is selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM. VU036172 (20 and 50 µM) prevents TNF-α and nitric oxide (NO) production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells.{47576} It reduces the expression of inducible nitric oxide synthase (iNOS) and increases the expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells when used at a concentration of 20 µM. VU036172 (50 mg/kg) reduces the size of cortical lesions, prevents neuronal degeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI), indicating improved recovery of motor function.  

 

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Description

A positive allosteric modulator of mGluR5 (Ki = 195 nM); selective for mGluR5 over mGluR1, mGluR3, and mGluR4 at 10 µM; prevents TNF-α and NO production by IFN-γ- or LPS-stimulated BV-2 and primary microglial cells at 20 and 50 µM; reduces expression of iNOS and increases expression of Ym1 and arginase 1 in LPS-stimulated BV-2 cells at 20 µM; reduces the size of cortical lesions, prevents hippocampal neurodegeneration, and improves sensorimotor deficits in the beam walk test in a mouse model of traumatic brain injury (TBI)

Formal name: N-cyclobutyl-6-[2-(3-fluorophenyl)ethynyl]-3-pyridinecarboxamide, monohydrochloride

Synonyms: 

Molecular weight: 330.8

CAS: 1309976-62-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Cell Biology|Cell Signaling|Nitric Oxide Signaling||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience|Neuroprotection

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