Home / TRPV Antagonists / GSK 2193874

GSK 2193874

Catalog #: 5106
9 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 (9)
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.

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:

9 Citations: Showing 1 - 9

  1. NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages.
    Authors: Neubert
    PLoS Biol  ;18
  2. Mechanical control of innate immune responses against viral infection revealed in a human lung alveolus chip.
    Authors: Girija Et al.
    Nat Commun  2022;13:1928
  3. Resident cardiac macrophages mediate adaptive myocardial remodeling.
    Authors: Sachio Et al.
    Immunity  2021;54:2072-2088.e7
  4. Evaluating methods and protocols of ferritin-based magnetogenetics.
    Authors: Miriam Et al.
    iScience  2021;24:103094
  5. Impaired TRPV4-eNOS signaling in trabecular meshwork elevates intraocular pressure in glaucoma.
    Authors: Yen-Lin Et al.
    Proc Natl Acad Sci U S A  2021;118
  6. Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice.
    Authors: Brant E Et al.
    Elife  2021;10
  7. Lipid Oxidation Induced by RF Waves and Mediated by Ferritin Iron Causes Activation of Ferritin-Tagged Ion Channels.
    Authors: Miriam Et al.
    Cell Rep  2020;30:3250-3260.e7
  8. A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis.
    Authors: Xu Et al.
    Oncotarget  2016;7:37622
  9. 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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