GSK2193874

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GSK2193874

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Cat No: 17715

Biochemicals - Ion Channel Modulation

GSK2193874 is a potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC50 values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively.{31400} It is selective for TRPV4 over ~200...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide

Correlated keywords:

1461716-89-1 TRPV4 GSK-634775 Ca GSK-2193874 TRPV-4 transient receptor potential cation channel vanilloid 4

Product Overview:
GSK2193874 is a potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC50 values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively.{31400} It is selective for TRPV4 over ~200 other human receptors, channels, and enzymes. GSK2193874 is effective in vivo, as it resolves pulmonary edema resulting from myocardial infarction in mice.{31400} TRPV4 blockade with GSK2193874 does not alter heart rate or blood pressure in rats, although it attenuates decreases in pulmonary and systemic arterial pressures induced by TRPV4 agonists.{31400,31399}

Size	1 mg
Shipping	dry ice
CAS Number	1336960-13-4
Molecular Formula	C₃₇H₃₈BrF₃N₄O
SMILES	BrC1=CC=C(C(C(NC2(CC2)C3=CC=CC=C3)=O)=C(CN4CCC(N5CCCCC5)CC4)C(C6=CC=CC(C(F)(F)F)=C6)=N7)C7=C1
Molecular Weight	691,6
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2933.39
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.