GSK 2193874

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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% (HPLC)
Citations (9)

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
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 Data for GSK 2193874

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

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for GSK 2193874

Certificate of Analysis / Product Datasheet
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References for GSK 2193874

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

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.

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9 Citations for GSK 2193874

Citations are publications that use Tocris products. Selected citations for GSK 2193874 include:

Sachio et al (2021) Resident cardiac macrophages mediate adaptive myocardial remodeling. Immunity 54 2072-2088.e7 PMID: 34320366

Brant E et al (2021) Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice. Elife 10 PMID: 34490843

Yen-Lin et al (2021) Impaired TRPV4-eNOS signaling in trabecular meshwork elevates intraocular pressure in glaucoma. Proc Natl Acad Sci U S A 118 PMID: 33853948

Miriam et al (2021) Evaluating methods and protocols of ferritin-based magnetogenetics. iScience 24 103094 PMID: 34622149

Do you know of a great paper that uses GSK 2193874 from Tocris? Please let us know.

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