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GSK2193874

Catalog No. T5640 CAS 1336960-13-4

GSK2193874 was identified as a selective, orally active TRPV4 blocker.

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GSK2193874, CAS 1336960-13-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 259.00
50 mg	In stock	$ 426.00
100 mg	In stock	$ 633.00
1 mL * 10 mM (in DMSO)	In stock	$ 113.00

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Purity: 98.79%

Purity: 98%

Biological Description

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Description	GSK2193874 was identified as a selective, orally active TRPV4 blocker.
Targets&IC50	TRPV4 (human):40 nM (IC50), TRPV4 (rat):2 nM (IC50)
In vitro	GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents[1,2].
In vivo	In isolated rodent and canine lungs, TRPV4 blockade prevented the increased vascular permeability and resultant pulmonary edema associated with elevated PVP. ?In both acute and chronic HF models, GSK2193874 pretreatment inhibited the formation of pulmonary edema and enhanced arterial oxygenation[2].
Animal Research	Adult male Sprague-Dawley rats (n = 7 to 8 per group) were treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg/day) via oral gavage for at least 4 days before osmotic challenges.?Rats underwent acute and chronic hyper- and hypo-osmotic challenges.Sprague-Dawley (control, n = 18) and spontaneously hypertensive rats (n = 11) were implanted with Data Sciences International (DSI) radiotelemetry transmitters.?Rats were dosed with GSK2193874, and data were captured with DSI receivers and analyzed with Microsoft Excel[2].

Molecular Weight	691.62
Formula	C37H38BrF3N4O
CAS No.	1336960-13-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (144.59 mM)

References and Literature

1. Cheung M , Bao W , Behm D J , et al. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4[J]. ACS Medicinal Chemistry Letters, 2017:acsmedchemlett.7b00094. 2. Thorneloe K S , Cheung M , Bao W , et al. An Orally Active TRPV4 Channel Blocker Prevents and Resolves Pulmonary Edema Induced by Heart Failure[J]. Science Translational Medicine, 2012, 4(159):159ra148-159ra148.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Inhibitor Library Orally Active Compound Library Anti-Cancer Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Ion Channel Inhibitor Library Bioactive Compound Library

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Related compounds with same targets

A-1165442 TRPM4-IN-2 Dihydrocapsaicin HC-030031 Fingolimod hydrochloride beta-Eudesmol M084 PF-04745637

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Keywords

GSK2193874 1336960-13-4 Membrane transporter/Ion channel TRP/TRPV Channel inhibit Transient receptor potential channels Inhibitor TRP Channel GSK-2193874 GSK 2193874 inhibitor

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