GSK 2193874
Tocris Bioscience, part of Bio-Techne | Catalog # 5106
Potent and selective TRPV4 antagonist; orally active
Key Product Details
Description
Potent and selective TRPV4 antagonist; orally active
Product Description
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 GlaxoSmithKlineProduct Specifications
Molecular Weight
691.62
Formula
C37H38BrF3N4O
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for GSK 2193874
For research use only
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