Home / TRPV Antagonists / GSK 2193874

GSK 2193874

Catalog #: 5106
3 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5106/25
5106/5
GSK 2193874 | CAS No. 1336960-13-4 | TRPV Antagonists
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Description: Potent and selective TRPV4 antagonist; orally active

Chemical Name: 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide

Purity: ≥98%

Product Details
Citations (3)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

GSK 2193874 is a potent and selective TRPV4 antagonist (IC50 values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca2+ influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.

Technical Data

M.Wt:
691.62
Formula:
C37H38BrF3N4O
Solubility:
Soluble to 50 mM in DMSO with gentle warming
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
1336960-13-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

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Citations for GSK 2193874

The citations listed below are publications that use Tocris products. Selected citations for GSK 2193874 include:

3 Citations: Showing 1 - 3

  1. NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages.
    Authors: Neubert
    PLoS Biol  ;18
  2. A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis.
    Authors: Xu Et al.
    Oncotarget  2016;7:37622
  3. Transient Receptor Potential Vanilloid 4 Ion Channel Functions as a Pruriceptor in Epidermal Keratinocytes to Evoke Histaminergic Itch.
    Authors: Chen Et al.
    J Biol Chem  2016;291:10252

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