GSK 2193874

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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
Datasheet
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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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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

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References

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


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Citations for GSK 2193874

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