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

VU0360172 (hydrochloride) – 5 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.  

 

Out of stock

Add to quotes
SKU: 22074 - Category:

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

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 10 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 10 mg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 mg

    Available on backorder

    Add to quotes
    View product page