GSK2193874
GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4[1].
Product Specifications
CAS Number
1336960-13-4
UNSPSC
12352005
Hazard Statement
H301, H315, H319, H335
Target
TRP Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
COVID-19-immunoregulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/GSK2193874.html
Purity
99.91
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(C1=C(CN2CCC(N3CCCCC3)CC2)C(C4=CC=CC(C(F)(F)F)=C4)=NC5=CC(Br)=CC=C15)NC6(C7=CC=CC=C7)CC6
Molecular Formula
C37H38BrF3N4O
Molecular Weight
691.62
Precautions
H301, H315, H319, H335
References & Citations
[1]Cheung M, et al. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. ACS Med Chem Lett. 2017 Mar 20;8 (5) :549-554.|[2]Thorneloe KS, et al. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4 (159) :159ra148.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
TRPV4
Available Sizes
Frequently Asked Questions
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