GSK 2193874

Name: GSK 2193874
Brand: Tocris Bioscience
SKU: 5106

Tocris Bioscience, part of Bio-Techne | Catalog # 5106

Citations (29)

COA / SDS

Potent and selective TRPV4 antagonist; orally active

Key Product Details

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% (HPLC)
Molecular Weight:	691.62

View Full Technical Details for GSK 2193874

Technical Data
Citations

Biological Activity for GSK 2193874

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries for GSK 2193874

GSK 2193874 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2193874

M. Wt	691.62
Formula	C₃₇H₃₈BrF₃N₄O
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1336960-13-4
PubChem ID	53464483
InChi Key	UIVOZBSCHXCGPS-UHFFFAOYSA-N
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 2193874

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	34.58	50 with gentle warming

Preparing Stock Solutions for GSK 2193874

The following data is based on the product molecular weight 691.62.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	2.89 mL	14.46 mL	28.92 mL
2.5 mM	0.58 mL	2.89 mL	5.78 mL
5 mM	0.29 mL	1.45 mL	2.89 mL
25 mM	0.06 mL	0.29 mL	0.58 mL

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References for GSK 2193874

References are publications that support the biological activity of the product.

Cheung Discovery of GSK2193874: an orally active, potent, and selective blocker of transient receptor potential vanilloid 4. ACS Med.Chem.Lett. 2017 PMID: 28523109
Thorneloe An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci.Transl.Med. 2012 PMID: 23136043