GSK 2193874

Pricing Availability Delivery Time Qty
Cat.No. 5106 - GSK 2193874 | C37H38BrF3N4O | CAS No. 1336960-13-4
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

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries

GSK 2193874 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 691.62
Formula C37H38BrF3N4O
Storage Store at +4°C
CAS Number 1336960-13-4
PubChem ID 53464483
Smiles O=C(NC6(CC6)C5=CC=CC=C5)C2=C(CN4CCC(N7CCCCC7)CC4)C(C3=CC(C(F)(F)F)=CC=C3)=NC1=CC(Br)=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
1eq. HCl 13.83 20
DMSO 34.58 50

Preparing Stock Solutions

The following data is based on the product molecular weight 691.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.45 mL 7.23 mL 14.46 mL
5 mM 0.29 mL 1.45 mL 2.89 mL
10 mM 0.14 mL 0.72 mL 1.45 mL
50 mM 0.03 mL 0.14 mL 0.29 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Product Datasheets

Safety Datasheet


References are publications that support the products' biological activity.

Thorneloe et al (2012) An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci.Transl.Med. 4 159 PMID: 23136043

Cheung et al (2017) Discovery of GSK2193874: an orally active, potent, and selective blocker of transient receptor potential vanilloid 4. ACS Med.Chem.Lett. 8 549 PMID: 28523109

If you know of a relevant reference for GSK 2193874, please let us know.

View Related Products by Target

View Related Products by Product Action

View all TRPV Antagonists

Keywords: GSK 2193874, supplier, GSK2193874, potent, selectiveTRPV4, inhibitors, antagonists, orally, active, transient, receptors, potential, vanilloids, channels, myocardial, infarction, pulmonary, oedema, edema, inhibits, TRPV, TRPV, Tocris Bioscience

Citations for GSK 2193874

Citations are publications that use Tocris products.

Currently there are no citations for GSK 2193874. Do you know of a great paper that uses GSK 2193874 from Tocris? If so please let us know.

Commented out for usability testing


TODO: Add Reviews

Literature in this Area


Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Pathways for GSK 2193874


TODO: Add Protocols