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GSK2798745

Cat. No. M14280

All AbMole products are for research use only, cannot be used for human consumption.

GSK2798745 Structure

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Quality Control & Documentation
Biological Activity

GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 is used in research for the treatment of pulmonary edema associated with congestive heart failure.

Chemical Information
Molecular Weight 460.53
CAS Number 1419609-94-1
Solubility (25°C) DMSO 150 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Brian G Lawhorn, et al. TRPV4 antagonists: a patent review (2015-2020)

[2] Carl A Brooks, et al. Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)

[3] Sarah Mole, et al. Investigating the effect of TRPV4 inhibition on pulmonary-vascular barrier permeability following segmental endotoxin challenge

[4] Joseph E Pero, et al. Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745

[5] Navin Goyal, et al. Clinical Pharmacokinetics, Safety, and Tolerability of a Novel, First-in-Class TRPV4 Ion Channel Inhibitor, GSK2798745, in Healthy and Heart Failure Subjects

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  Catalog
Abmole Inhibitor Catalog




Keywords: GSK2798745 supplier, TRP Channel, inhibitors, activators

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